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R. Kiplin Guy St. Jude Children’s Research Hospital (SJCRH)

Department of Chemical Biology and Therapeutics

Curriculum Vitae

CURRENT TITLE AND DEPARTMENT Chairman and Member, Department of Chemical Biology and Therapeutics, SJCRH

Robert J. Ulrich Endowed Chair in Chemical Biology and Therapeutics, SJCRH

SECONDARY APPOINTMENTS, Adjunct Professor of Pharmaceutical Chemistry, University of California San Francisco (UCSF)

Adjunct Professor of Biochemistry, Vanderbilt University Adjunct Professor of Pharmaceutical Sciences and Pathology, University of Tennessee

EDUCATION

1996-1998: University of Texas Southwestern Medical Center (UTSWMC) Dallas, TX Postdoctoral Fellowship in Cellular Biology with Drs. Brown and Goldstein 1991-1996: The Scripps Research Institute (TSRI) La Jolla, CA Ph.D. in Organic Chemistry with Dr. K. C. Nicolaou 1995 The Woods Hole Research Institute Woods Hole, MA Physiology: Cellular and Molecular Biology Course 1986-1990: Reed College Portland, OR B.A. in Chemistry

ACADEMIC AND PROFESSIONAL POSITIONS 1990-1991: Contract Chemist, IBM-Almaden Research, San Jose, CA 1998-2005: Assistant Professor, Department of Pharmaceutical Chemistry, School of Pharmacy and Department of Cellular and Molecular Pharmacology, School of Medicine, UCSF, San Francisco, CA 1998-2005: Member, UCSF Comprehensive Cancer Center Genitourinary Program (now Breast Oncology and Prostate Cancer Programs) 1998-2005: Member, Cardiovascular Research Institute, San Francisco, CA 2000-2005: Founding Member, QB3 Institute (quantitative biology), San Francisco, CA 2002-2005: Director, Center for Chemical Diversity, San Francisco, CA 2003-2005: Executive Director, Bay Area Screening Center, San Francisco, CA 2005: Professor (direct promotion from Assistant Professor), Department of

Pharmaceutical Chemistry, School of Pharmacy and Department of Cellular and Molecular Pharmacology, School of Medicine, UCSF, San Francisco, CA

2005-present: Member and Chairman, Department of Chemical Biology and Therapeutics, SJCRH, Memphis, TN

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SPECIALTY; SUBSPECIALTY Specialties Chemical biology, preclinical drug discovery and development Subspecialties Medicinal chemistry: hit-to-lead and lead optimization; initial animal studies Synthetic organic chemistry: synthesis of terpenes and peptides, parallel and combinatorial synthesis, laboratory automation Cellular biology: lipid homeostasis, nuclear hormone receptors, protein interactions Cancer biology: Breast, prostate, brain, and developmental tumors of children Parasitology: malaria and human African trypanosomiasis High-throughput screening: quantitative assays, high-content methods, cell morphology, data analysis methods

MEMBERSHIPS IN SCIENTIFIC, PROFESSIONAL, AND SCHOLARLY SOCIETIES American Chemical Society, American Society for Cell Biology, Society for Biomolecular Sciences, American Association for Cancer Research, and American Society for Biochemistry and Molecular Biology

RESEARCH AND CREATIVE ACTIVITY Target Validation, Lead Discovery, and Lead Optimization for Neglected Diseases My group focuses on the discovery and preclinical development of new therapeutic leads for neglected diseases. We place a major focus on discovering new therapeutic chemotypes, determining their mechanism of action, and conducting proof-of-concept studies in pharmacokinetic/pharmacodynamic (PK/PD) models of disease. All of the projects are intended to deliver well-validated compounds that have suitable pharmacokinetic and toxicology profiles for detailed in vivo studies. During my independent career, both historically and currently, the projects in my laboratory have been split roughly equally between oncology and protozoal diseases. The details of each program are outlined below.

Research Projects in Pediatric Oncology 1. A phenotypic approach targeting oncogenic mutations for pediatric brain tumors In 2007 we established a collaboration with physician scientist Richard Gilbertson in order to address the paucity of novel targeted therapies for pediatric brain tumor trials. We built a working group including basic scientists, chemical biologists, medicinal chemists, pharmacists, pharmacologist translational scientists, and physicians. In this collaboration we have used whole-cell phenotypic screening approaches in murine genetic models to discover chemical suppressors of oncogenes that induce pediatric brain tumors, including ependymomas and choroid plexus carcinomas. Ependymomas are a pediatric brain tumor that affects about 200 new patients per year and causes about 50 deaths per year. There are currently no efficacious standard chemotherapy

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approaches for ependymomas. We have a research consortium for ependymoma funded by the CERN foundation (Collaborative Ependymoma Research Network). In this effort, Dr. Gilbertson’s laboratory has identified a set of well-validated oncogenes using a murine transplantation model that tests radial glial cells (the precursors for ependymomas)1, 2, which have been virally transduced with the putative oncogene. He has shown that this progenitor cell population can establish a pathologically appropriate tumor when injected into an intact animal. Cells derived from animals expressing bona-fide oncogenes were used to set up a differential cell-killing assay using a mixture of the population expressing the oncogene and cells of the same lineage not expressing the oncogene. A key aspect to this effort was the use of 3D culture methods, namely neurospheres, which ensured the cells maintained a proper physiological state and sensitivity to standard of care drugs. To date we have carried out screens with two cell lines: one, over expressing the EphB2 receptor, and the other, over expressing Notch. In working with the EphB2 system, we tested all FDA-approved drugs and identified a lineage-specific sensitivity to agents that perturb folate metabolism, including both 5-flurouracil (5-FU)

and methotrexate, as well as sensitivity to other agents, especially bortezomib and

gemcitabine. Subsequent in vivo experiments with 5-FU confirmed this activity in tumor models. Currently, PK/PD modeling studies are underway to optimize for dosage and schedule for the other drugs.3 A phase 1 trial has been completed with 5-FU4 and a Phase 2 trial is under review. A phase 1 trial with gemcitabine is also currently under review. Using the same screening system we tested a wide range of kinase inhibitors from

the publically available GSK and Roche tool sets, as well as a collection of commercially available kinase inhibitors. This study revealed that the PLK1 kinase inhibitors were highly active.3 Because PLK1 inhibitors are poorly distributed into the brain and systemically toxic, we have an ongoing chemistry program for improving blood brain barrier (BBB) penetration. We are also developing a local delivery approach for PLK1 inhibitors. Next, we used the EphB2 system to screen a large collection of natural product extracts and identified some novel chemical leads5, which we plan to pursue in the near future. Finally, in comparing pharmacological sensitivity patterns, we showed a high degree of similarity in sensitivity patterns between the

Priority novel chemotypes for pediatric brain tumors

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ependymoma. Therefore, we tested the hits identified in the choroid plexus carcinoma (CPC) screen described below and identified three hit series (see figure), which are the focus of our current lead optimization efforts. Choroid plexus carcinomas (CPC) are a rare brain tumor affecting less than 50 patients per year that have no standard of care. For CPC, we have followed a similar approach, this time using a choroid plexus specific Pten/p53/RB knockout mouse. This mouse produces a moderate penetrance tumor that appears to be a true choroid plexus carcinoma. Once the tumor was established, we were able to serially passage the tissue in recipient mice, generating multiple sub-models. We have followed the same paradigm as with ependymoma in looking at potential drugs for repurposing. Gemcitabine and clofarabine are the two most promising candidates, with phase 1 trials under review. With the CPC model, we can generate many more cells than with the ependymoma model and for this reason have carried out a whole cell phenotypic screen of the entire St. Jude collection (~1.2 million compounds), which has generated several thousand hits that either induce differentiation, cause cell stasis, or kill the tumor cells. The optimization of these leads and the identification of their targets will be a major focus in the laboratory for the next five years (see below for an example of hit optimization for malaria). We have also recently established projects following the same general paradigm (although working with human tumor derived samples in addition to murine models) for medulloblastoma and high grade gliomas, which affect roughly 500 and 100 patients per year, respectively. The medulloblastoma project is a collaboration with Martine Roussel’s laboratory and the glioma project a collaboration with Suzy Baker’s laboratory

2. A structure based approach to targeting MDMX activity for retinoblastoma Retinoblastoma (RB) is a solid tumor of the eye that affects about 300 patients per year. Although the cure rate is very high, exceeding 90%, treatment often requires removal of the eye. We have focused on identifying therapies that would either allow delaying enucleation or remove the need for enucleation in some cases. In order to reduce the delayed effects of treatment for retinoblastoma, a pediatric ocular tumor, we established a collaboration between our group, led by Michael Dyer, PhD, a developmental biologist who models retinoblastoma, and Rachel Brennan, MD, a physician scientist. This project was based on our prior work on targeting

Nutlin-3a and analogs developed for retinoblastoma.

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MDM2.6 We discovered that amplification of MDMX is a major driver of retinoblastoma and that the Roche drug Nutlin-3a, which targets MDM2, also works, albeit poorly, on MDMX.7 Early in our project, Roche pulled nutlin-3 from development in favor of RG7112, a second generation compound, due to hematological toxicity observed in the clinic. We demonstrated that local delivery of nutlin in preclinical models gave good efficacy without this toxicology, but its bioavailability and potency on MDMX were not optimal.8 Analysis of both the IP landscape and the binding mode of Nutlin-3a to MDMX allowed us to target novel nutlin analogs that were predicted to have better binding to MDMX, but were not covered by Roche patents. Recognizing that existing methods for synthesis were quite poor with respect to enantioselectivity, we leveraged the expertise of the Johnston group at Vanderbilt University (Nashville, TN). This collaboration led to the development of roughly ten compounds (see figure) with significantly increased affinity for MDMX and decreased affinity for MDM2.9 Using pharmacokinetic models we were able to show that achievable concentrations for these compounds in the eye after local delivery were comparable with nutlin and well within efficacious levels. Systemic exposure, as targeted, is now minimal. We are currently studying these molecules in retinoblastoma efficacy models. The findings of this project has led to the formation of a new company, Focal Point Therapeutics, which is focused upon development of these analogs for RB and proliferative vitreoretinopathies. . Finally, we have completed a high throughput screen for novel chemotypes blocking the interaction of MDMX and p53,10 using a protein interaction assay. While we identified a number of new inhibitors, we feel the quality of the hits is not to our standard11. Therefore, we are exploring a cellular assay for the in situ interaction of the two proteins and/or structure-based design to generate backup candidates. 4. Targeting the DCN1-UBC12 interaction for carcinomas. SCC including those of the lung, esophagus, and head and neck, cause over one third of cancer-related deaths.12-14 with poor survival rates (ca. 16% for lung)15 Thus, there is a pressing need to develop novel approaches to treat SCC. DCN1 is amplified in >40% of lung SCC and associated with malignant transformation, metastasis, and poorer patient survival rates.16-19 DCN1 binds to the acetylated N-terminus of UBC12 (an E2 enzyme for the ubiquitin-like protein (UBL) NEDD8) and the “Cullin (or CUL)” family of proteins to act as a co-E3 promoting NEDD8 modification of CULs which activates them to regulate ubiquitination of a wide range of clients20-23. We have started a collaboration with Brenda Schulman’s laboratory at St Jude (discoverer of the DCN mechanism) and Bhuv Singh’s laboratory at MSKCC (Discoverer of DCN1) to discovery inhibitors of the DCN1-UBC12 interaction. Their studies show that DCN1 activity depends on a ≈350 Å3 pocket in the DCN1 oncoprotein binding to UBC12’s acetylated N-terminal methionine23, 25, 26.

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We developed a biochemical screening method based on the crystal structure constructs and

screened 598,533 unique chemicals at a single concentration of 30 µM (see figure). 856 active compounds (>45% activity, 0.15% hit rate) were validated revealing 107 compounds with potency (IC50) less than 10 µM that assorted into three series. Series 1 is contains a N-benzyl (or benzoyl) piperidine core (SJ212329), series 2 a pyrazolylpyrimidine core (SJ347815), and series 3 a pyrazolopyridineone core (SJ400727). These series also inhibited DCN1 NEDD8 transfer to cullins in the context of a full cullin-RING E3 with potencies similar to those blocking interactions. Inhibitor-DCN1 X-ray Optimized DCN1 inhibitor

Novel inhibitors of the DCN1-UBC12 Interaction. Data for series are color matched to structures. A) Representative analogs from each series. B) Dose-dependent inhibition of the DCN1-UBC12NAc interaction as measured by TR-FRET. C) Dose-dependent inhibition of [32P]~NEDD8 transfer from UBC12 to CUL2CTD-RBX2, as measured by pulse-chase. D) Superimposition of X-ray crystal structures (1.7-2.0 Å res) of DCN1 (gray) bound to UBC12NAc (magenta) or representative members from each series (orange, green cyan). All three series occupy the targeted binding pocket. E) Cell viability assay for lung tumor lines expressing high levels of DCN1 (HCC95) or low levels of DCN1 (H2170).

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crystal co-structures were determined for each series, revealing our compounds bind to the targeted UBC12 N-acetyl methionine binding pocket23, 25, 26. The series were non-toxic to wild-type (wt) fibroblasts (BJ cells) and a representative of Series 1, SJ212329, was slightly more potent against cells with high DCN1 (HCC95) than relatively low DCN1 (H2170) as desired. We have used structure based approaches to optimize Series 1 which has led to the development of a potent compound (80 nM) with cellular activity. We are currently studying the effects of this compound on cells, its selectivity, and effects on ubiquitinated protein pools.

4. Targeting the differentiation block in alveolar rhabdomyosarcoma We have recently started a project targeting relief from the developmental block that characterizes alveolar rhabdomyosarcoma. This block is induced by the expression of the PAX-FOXO transcription factor fusion proteins that characterize the disease genetically. In collaboration with Mark Hatley, in Oncology at St Jude, who is an expert in muscle development, we have developed cellular models for monitoring restoration of normal muscle cell differentiation in alveolar rhabdomyosarcoma (ARMS) cells and have shown that phorbal esters such as TPA partially induce differentiation. We are currently pursuing two approaches with this system: 1) identification of the downstream mediators of the TPA-induced signal to determine if there are key drivers (e.g., kinases) that could be targeted; and 2) use of the cell model to carry out a high throughput phenotypic screen for inducers of differentiation.

Research Projects in Neglected Protozoal Infectious Diseases 1. Phenotypic approaches to lead discovery and optimization of antimalarial compounds Malaria is a disease that affects several hundred million patients a year and kills well over 500,000 children every year. While there are some effective therapies, resistance is emerging to all current drugs. New classes of drugs are urgently needed. An additional need is safe drugs that block the transmission of malaria and thus reduce population burdens of the disease. In the past 10 years my group has published a number of papers on lead optimization of antimalarial compounds with leads arising either from known antimalarial chemotypes or from targeted screens of drug libraries. A thorough survey of literature revealed to us that antimalarial research efforts had explored a very small chemical landscape and yielded only a few well-validated targets. This survey of over 800 papers has been published as a chapter in the new Burger’s Medicinal Chemistry27 and a Chemical Reviews manuscript.28 We concluded that existing

Antimalarial Lead Series Arising from Screen

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targets and chemotypes had been exhausted, thus meaningful progress would require new discoveries in either area. This thinking led us to develop a method for of large libraries for antimalarial activity, regardless of mechanism of action. We executed a whole-cell phenotypic high throughput screen of over 1.2 million compounds to identify novel chemicals that kill the malaria parasite. Then, I established collaborations with 12 other groups world-wide, including basic researchers, physicians, and clinicians. We evaluated the hits from the screen to establish mechanism of action, examine cross-activity with other protozoa, and evaluate tractability for development, which we published in Nature.29 Next, I redirected our collaborative efforts to drug development and lead optimization. The consortium was funded by the Medicines for Malaria Venture and the NIH. Three lead series from this work (see figure) are currently in development: the dihydroisoquinolones (DHIQ’s), dihydropyridines (DHP’s), and diaminonapthoquinones (DANQ’s). The most advanced series from this effort is the DHIQ’s, which have recently led to a clinical candidate, SJ000557733, being approved for development by Medicines for Malaria Venture (MMV). The development and mechanism of this series were described in a recent PNAS paper.30 I assembled a collaboration between my group, the St. Jude Clinical group, the Medicines for Malaria Venture, and Eisai Pharmaceuticals in order to develop (+)-SJ000557733 and this project is now funded by the Global Health Innovative Technology Fund through completion of Phase 1. (+)-SJ000557733 has good potency in vitro with an EC50 = 23 nM and maintains similar potency against all resistant strains tested to date. (+)-SJ000557733 is highly efficacious against P. falciparum in vivo with an ED90 = 1.7 mg/kg, significantly superior to the standard of care antimalarial drugs chloroquine and comparable to artesunate and pyronaridine. Pharmacokinetic studies in mice, rats, and dogs have shown the compound to be well absorbed, with 60-100% oral bioavailability and reasonable clearance. In vivo studies have demonstrated clear potential for transmission blocking through activity on the sexual stages of the parasite. The compound is very well tolerated in vivo with no major toxicological liability based on in vitro and in vivo studies. Comparison of efficacious doses in the mouse with the results from a 7-day toxicology study in the rat predicts at least a 60-fold safety margin for (+)-SJ000557733. We have recently shown that (+)-SJ000557733 selectively induces eryptosis in infected red cells by inhibiting a parasite protein PfATP4. Consistent with the other PfATP4 inhibitor to enter clinical development (KAE609), (+)-SJ000557733 demonstrates a fast kill rate in vivo that is identical with artesunate. These data demonstrate (+)-SJ000557733 to be an efficacious, safe, and clinically relevant anti-malarial agent. An investigational new drug application (IND) to the FDA was filed in October 2015 and we anticipate human trials to commence in Q1 2016, in partnership with Eisai. We have recently begun optimizing the DHP compound series. Preliminary data indicate that this series is potent, fast acting, and acts by a novel, as yet unidentified, mechanism. Current efforts are focused on understanding the drivers for bioavailability, identifying the mechanism, and studying the leads in pharmacodynamic models. We are also beginning to work up other series discovered in the screen. 2. Lead Discovery for human African trypanosomiasis (HAT)

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Human African Trypanosomiasis (HAT) affects roughly 10,000 patients per year and is uniformly fatal if not treated. While much progress has been made in the past decade, the current standard of care drugs are still poorly tolerated, efficacious only on subsets of the parasite causing the disease, and subject to resistance. Therefore there is a need for novel targeted therapies. Our past efforts in HAT focused on TbCatB, a cathepsin B homolog essential for normal parasite growth. We identified a purine nitrile inhibitor that selectively targets the protozoal enzyme and has good potency and good correlation between cellular and enzyme models. The most advanced candidate was orally available, had good BBB penetration, and was efficacious in vivo against the cattle pathogen (T. brucei brucei), the standard disease model. Unfortunately, it was not equally efficacious against the dominant human pathogen, which we showed was due to species differences in enzyme utilization. We have now dropped this project. We recently discovered a new series of anti-trypanosomal leads using whole-cell screening. The leads from this screen have reasonable bioavailability and activity in vivo; the mechanism of action is unknown. We are evaluating a small set of optimized lead analogs for mechanism of action and potential for further development. RESEARCH AWARDS, FELLOWSHIPS, AND EXTRAMURAL GRANTS Summary:

I have raised a sum total of roughly 29 million dollars in direct funding from a variety of sources, including private foundations, NIH, National Science Foundation (NSF), and the Department of Defense (DOD). Current grants include one R01 as a Co-PI; a grant from CERN for ependymoma; and a grant from Global Health Innovative Technology (GHIT) for clinical development of DHIQs for malaria. In addition, I have mentored graduate and postdoctoral fellowships from external agencies for a total of $360,000. Prior Funding: 3/1/99: PI, UCSF Academic Senate, “Shared Equipment Grant for Parallel Synthesis Apparatus,”

$29,700 total direct funding. 11/98-11/99: PI, UCSF Academic Senate, “Inhibition of hTRß1/GRIP1 Binding,” $30,000 total

direct funding. 7/99-7/00: PI, UCSF Cancer Center, American Chemical Society (ACS) Award, Inhibition of

p53/mdm2 binding, $20,000 total direct funding. 7/99-7/00: PI, Sandler Program in Basic Sciences, Alpha Helical Mimetics, $50,000 total direct

funding. 7/98-7/00: PI, Sidney Kimmel Foundation for Cancer Research, Structural Proteins as Drug

Targets, $173,000 total direct funding. 6/00-5/03: Mentor, Department of the Army, Breast Cancer Research Program Pre-Doctoral

Traineeship for Timothy Geistlinger, “Evaluation of the Estrogen Receptor•Coactivator interface as a Target for Breast Cancer Chemotherapeutic Drug Design,” $65,523 total direct funding.

7/00-6/01: Co-PI, Sandler Program in Basic Sciences, MS-3D: Low Resolution Protein Structure by Chemical Crosslinking and Mass Spectrometry, $100,000 total direct funding.

7/00: PI, UCSF REAC “Purchase of a Shared High Throughput Fluorescence Polarization Platereader,” $60,000 total direct funding.

7/00-6/01: Mentor, California Breast Cancer Research Program Postdoctoral Fellowship for

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Thomas Robertson, “A New Class of Drugs to Treat Breast Cancer,” $40,000 total direct funding.

9/00-8/01: Investigator (PI B. Gibson), NIH 1 S10 RR14601-01, “LCQ-Deca Ion-Trap HPLC/MS System,” $261,890 total direct funding

9/1/00-8/31/01: PI, NIH R55 DK58080-01 (J. A. Shannon Director’s Award), “Novel Inhibitors of Nuclear Receptor Function,” $80,000 total direct funding.

4/01-3/02: PI, Sandler Program in Basic Sciences, Seed Grants for Priority Basic Science Projects, “A Facility for the Parallel Synthesis, Purification, and Characterization of Combinatorial Libraries of Discrete Substances,” $416,000 total direct funding

5/01-4/02: Co-PI (with Joe DeRisi), Sandler Program in Basic Sciences, “Genomic Structure Activity Relationships,” $46,000 total direct funding

6/01-5/02: Co-PI (with Robert Fletterick), UCSF Prostate Cancer Research Program, “Novel Inhibitors of Androgen Receptor Function,” $50,000 total direct funding

1/02-12/03: Co-PI (with Robert Fletterick), CAPCure, “Novel Inhibitors of Androgen Receptor Function,” $100,000 total direct funding

7/02-6/03: PI, UCSF Stewart Trust, “Chemical Genetics of PDZ Domains,” $50,000 total direct funding

6/00-5/04: PI, NSF-CHE 9984227, “Total Synthesis of Phalloidin and Amanitin,” $360,500 total direct funding.

6/01-5/04: Mentor, Department of the Army, Breast Cancer Research Program Pre-Doctoral Traineeship for Jamie Moore, “Structure and Dynamics of Nuclear Receptor Coactivator Interactions,” $65,523 total direct funding.

6/02-5/04: Co-PI with Robert Fletterick, NIH R21 CA095324, “Inhibition of Androgen Receptor Activation,” $200,000 total direct funding

4/02-3/04: PI, Cystic Fibrosis Foundation Guy02x0, “Medicinal Chemistry for Cystic Fibrosis Drug Discovery,” $81,000 total direct funding

4/02-3/05: Project Co-Director (with Cliff Berkman, San Francisco State University and Charles Craik, UCSF), PI Mac Roach, UCSF, NIH U56 CA096216, “Combinatorial Approaches for Studying Substrate Recognition and Developing Inhibitors of PMSA,” $96,000 total direct funding

8/00-7/05: Core C Co-Director (PI, Robert Fletterick), NIH-National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) DK58390-01, “Structure and Dynamics of Nuclear Receptors,” $3,471,937 total direct funding; $888,614, total direct Core C funding.

1/04-12/04: PI, Prostate Cancer Foundation, “Novel Inhibitors of Androgen Receptor Funding,” $75,000 total direct funding

1/04-1/06: PI, QB3 Opportunity Award, “Bay Area Screening Center,” $120,000 total direct funding

4/04-4/06: PI, Sandler New Technologies Fund, “Bay Area Screening Center,” $690,000 total direct funding

6/04-6/06: PI, School of Pharmacy Dean’s Account, “Bay Area Screening Center,” $120,000 total direct funding

8/04-8/06: PI, Buck Institute, “Bay Area Screening Center,” $120,000 total direct funding 7/01-6/06: Chemistry Core Director (PI, James McKerrow), Sandler Program in Basic Sciences,

“Basic Research in Parasitic Diseases,” $560,000, total direct Core C funding. 9/01-8/06: PI (co-investigators I. D. Kuntz and B. Gibson), NSF Division of Chemistry

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“Moderate Resolution Protein Structures by Chemical Crosslinking and Mass Spectrometry,” $1,333,000 total direct funding

9/02-8/07: PI, NIH 5 U01 AI053862 “Novel Anti-Malarials by Combinatorial Pharmacogenomics,” $2,500,000 total direct funding

3/08: PI, Tayebati Foundation, $1,000,000 5/07: PI, Barbara Ann and Zach Wylde Foundation, $1,000,000 9/02-8/07: Co-Director Chemistry Core, NIH 2 P01 GM56531-06, “Structure, Biology, and

Targeted Drug Design AIDS,” $7,500,000 total direct funding, $1,500,000 total direct funding (Core C).

12/02-11/07: Project PI, NIH P01 AG021601 “Novel Therapeutics for Prion Disease,” $20,800,000 total direct funding, $1,700,000 Core C Total Direct Funding.

12/06-12/08: Postdoctoral Fellowship (Feau, C, PI), DOD, “Novel Small Molecule Antagonists of the Interaction of the Androgen Receptor and Transcriptional Co-Regulators,” $111,367 total direct funding.

8/07-7/12: PI, U01AI075517, “Development of Antimalarial Preclinical Candidates” $5,204,090 total direct funding. 9/01-8/13: PI, NIH R01 DK58080, “Novel Inhibitors of Nuclear Receptor Function, $1,345,277

total direct funding – no-cost extension 9/10-9/13: Co-PI; DoD CA093469P2; “Chemotherapeutics for Choroid Plexus Carcinomas,”

$343,162 Guy laboratory total direct costs. Active Funding: 7/08-6/16: PI, 180942020, “CERN P3: Molecular Targeted Drug Development” $1,246,052 total direct funding. 9/11-9/16: Co-PI, R01AI090662; “Lead Optimization for Antimalarials,” $3,549,870 total direct

funding. 9/14-9/16: PI, GHIT Grant, “Preclinical and Clinical Development of the DHIQ’s” 3,800,000

total direct costs

HONORS AND AWARDS 86-90, annually: Commended by the Reed faculty for academic excellence 8/86-5/90: John Hauberg Scholarship 6/90: American Institute of Chemists Student Award 6/90: Phi Beta Kappa 8/91-6/94: Office of Naval Research Graduate Fellowship 4/94: Arthur Scott Lecturer, Reed College 6/94: Roche Award for Excellence in Organic Chemistry 6/94-6/95: American Chemical Society - Organic Chemistry Graduate Fellowship 6/95-8/96: George Hewitt Medical Research Foundation Fellowship 9/96-9/98: The Helen Hay Whitney Postdoctoral Fellowship 7/98-7/00: Sidney Kimmel Cancer Research Foundation Scholar 6/00-5/04: NSF CAREER Award 3/08: Robert J. Ullrich Endowed Chair in Chemical Biology and Therapeutics 5/08: Walter Reed Army Institute of Research Honorary Lecturer 9/09: Memorial Sloan Kettering Cancer Center Honorary Lecturer 8/10: Mentor of the Year, SJCRH

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TEACHING I currently teach at UCSF for one week of lectures in the winter quarter. My prior teaching

experience is outlined below. Formal Scheduled Classes for UCSF Students

Academic Year and Quarter

Course Number

Course Title Nature of Contribution

Hrs/Qtr of Instruction

Total Students Enrolled

1999-2005 Fall

PC 121 Endocrine and Immunologic Agents

Instructor (1999-) Course Director (2004-

Eight hours of lecture (1999-203) 22 hours of lecture (2004-

125

2000 Fall

Biochem 200A

Macromolecules Discussion Group Leader

20 hours of conference

10

1999-2005 Winter

PC 242 Bioorganic Chemistry

Instructor (1999-2002; 2004-) Course Director (2000-)

20 hours of lecture

10-15

1999-2001 Spring

PC 203 Synthetic Organic Chemistry

Instructor Five to15 hours of lecture

5-10

2010-present Winter

-- Chemical Biology Instructor Five hours of lecture

5-10

Short Courses

Academic Year and Quarter

Course Title

Nature of Contribution

Location Hrs/Qtr of Instruction

Total Students Enrolled

2004-2005 Summer

Chemical Genetics

Course Director (2004-) Instructor (2004-)

Gulbenkian Institute (Portugal)

Eight hours of lecture

14

2006-2009 Summer

Biology of the Parasite

Instructor Woods Hole Marine Biology Laboratory

Three hours of lecture

16

2009-2010 Spring

Medicinal Chemistry Workshop

Instructor Cape Town Two hours of lecture

30

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MENTORING I remain actively involved in direct teaching and mentoring of students, postdoctoral

fellows, and junior faculty. My mentoring efforts are outlined below.

Summer Research Students: Name Summer School Project

Thuy Vo 1999 UC - Berkeley Synthesis of a Spin Label Analog to FLASH Allison Chambers 2000 CSU – Bakersfield Synthesis of 2-Carboxyindoles Chinedu Mmeje 2001 UC - Santa Barbara Synthesis of Estrogen Receptor and Thyroid

Receptor Selective Peptides LaWanda Johnson

2002 Fort Lewis College Mass Spectrometry in Three Dimensions

Sarah Chui 2003 UC – Berkeley Expression of LXRα Lillian Seu 2004 Barnard Synthesis of Biaryl Ethers Christina Roels 2006 Whitman Synthesis of KSHV Protease Inhibitors Richard Miskimins

2007 Brigham Young University – Idaho

Assembly of an FDA-Approved Drugs Library for High-Throughput Screening for Glucocorticoid Receptor Agonists Using a Specific Bioactive Compound Library

Michelle Paul 2008 2009

Christian Brothers University

Identification Of Synergistic Antimalarial Drugs

Kristin Brown 2009 Baylor University Evaluation of Pre-fractionated Natural Products Extracts as Antimalarials

Elizabeth Jeans 2009 Rhodes College Construction of an Exhaustive Antimalarial Database

Yandira Salinas 2010 -- Annotation of Drugs with Target in a Bioactives Database

Nicholas Patel 2011 University of Wisconsin

Pharmacokinetics of Dihydroisoquinolines

Karina Mendoza 2012 California Polytechnic State University

Synthesis of Antimalarial Diaminonapthoquinones

Katelyn Rittenhouse

2012 Eastern University Synthesis of Diaryl Urea Inhibitors of the Interaction of the Androgen Receptor and FKBP

Richard Barrios 2013 Florida International University

Cell Biology of DANQs, a Potential Survivin Inhibitor Active Against Malaria.

Vanesssa Juettner 2013 University of Illinois – Chicago

Pharmacokinetics of a New Series of Anti-Trypanosomal Compounds

Richard Barrios 2014 Florida International University

Induction of DNA Damage by DCN1 Inhibitors

Shannon Zhang 2014 Yale University Developing a Method for High-Content Screening for Induction of Differentiation in

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Rhabdomyosarcoma Cells Alexandria Vazquez-Salgado

2015 University of Puerto Rico

Mechanistic Characterization of Cell Cycle Arrest in Trypanosomes by Novel Inhibitors

Masters Dissertations Completed under Mentorship

Name Years in Lab

Program Project

Ian Maulhardt (Co-supervised with Joe DeRisi) Terminal Masters Degree

1999-2001 UCSF Pharmaceutical Chemistry

Genomic SAR of Benomyl

Gerlof Kruidhof (Co-supervised with B. Feringa)

2002 U. Groningen Chemistry

Alpha Helical Peptidomimetics

Sabina Gerber 2002-2003 U. Strasberg Parallel Synthesis of Phenothiazines

Florent Ubelman 2007 Institut Curie Development of a Novel Reporter System for Thyroid Hormone Receptor Function

Thaiz Rivera Vargas 2008 Universite Paris Diderot

Development of a Novel Reporter System for Thyroid Hormone Receptor Function

Nathalie Ingouf 2009 Universite Paris Diderot

Evaluation of Synergistic Pairs Among FDA Antimalarials

Djihad Hajid 2013 Universite Paris Diderot

Development of Methods for Establishing Mechanism of Action for Hits from Whole Cell Screens

Mariell Pettersson 2014 Goteborg University

Development of Inhibitors of the p53-MDM2 Protein Interaction

Britanny Greenberg 2014-2015 University of Tennessee

Differentiation Therapy for Rhabdomyosarcoma

Doctoral Dissertations Completed under Mentorship

Name Years in Lab

Program Project Current Position

Timothy Geistlinger (DOA-BCRP Pre-Doctoral Fellow)

1998-2004

UCSF Chemistry and Chemical Biology (CCB)

Inhibition of NR•p160 Binding

Vice President of R&D, Beyond Meat

Kathleen Pendola 1999-2004

UCSF PC Inhibition of PDZ Domain Ligand Interactions

Clinical Pharmacist, Beth Israel

Jamie Moore (DOA-BCRP

2000-2004

UCSF CCB

Structure and Dynamics of Nuclear Receptor

Director, Late Stage Pharmaceutical Development,

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Pre-Doctoral Fellow)

Coactivator Interactions Genentech

Felice Lu (Co-supervised with Tack Kuntz)

2000-2005

UCSF CCB

Design and Synthesis of Inhibitors of the Interaction of p53 and mdm2

Research Policy Manager, University of California Office of the President

Peter Madrid 2001-2005

UCSF CCB

Parallel Synthesis of Quinolines

Director of Discovery Technologies, SRI International

Anang Shelat (Co-supervised with Tack Kuntz)

2001-2005

UCSF CCB

Automated High Throughput Data Mining

Assistant Member, SJCRH

Nicholas Mills 2003-2007

UCSF CCB

Applications of Constrained Alpha Helical Peptides

Partner, McKinsey and Company

Jeremy Mallari 2004-2008

UCSF CCB

Synthesis of Antiprotozoal Cysteine Protease Inhibitors

Assistant Professor of Chemistry, California State University San Bernadino

David Smithson 2004-2009

UCSF CCB

Synthesis of Antiprotozoal Aspartyl Protease Inhibitors

Scientist, Genentech

Samantha Cooper 2004-2009

UCSF BMI

Circuit Analysis of Nuclear Hormone Receptor Responses

Computational Biology Group Manager, Bio-Rad

Yandira Salinas 2014- UTHSC Acquisition of Drug Resistance in Malaria and Pediatric Tumors

--

Professional Research Personnel

Name Years in Lab Title Current Position Edward Olsen 1998-1999 Laboratory Helper, UCSF Neurologist, Vancouver WA Karen Tuttle 1999-2000 Laboratory Helper, UCSF Unknown Sarah Galicia 2001-2003 Junior Specialist, UCSF Manager, Prevention and Cancer

Screening Program, Central East Regional Cancer Program, Ontario

Andrea McReynolds 2001-2005 Staff Research Associate I, UCSF

Unknown

Daniel Grundig 2002 Staff Research Associate, UCSF

Research Associate, Berlex

Kim Carter 2003 SFWorks Intern, UCSF Staff Research Associate, UCSF Valerie Smith 2003 SFWorks Intern, UCSF Student, City College of San

Francisco (CCSF) John Sherrill 2003-2005 Junior Specialist, UCSF Senior Research Associate,

SAMDI Tech Naoaki Fujii 2002-2005 Professional Researcher,

UCSF Associate Member, SJCRH

Martina Sigal 2003-2005 Specialist, UCSF Laboratory Supervisor, SJCRH

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2005- Janice Williams 2003-2005 Specialist, UCSF Senior Scientist, Presidio

Pharmaceuticals Ovidio Velasquez 2004 SFWorks Intern, UCSF Analyst 1, UCSF Abdul Mahrat 2004 SFWorks Intern, UCSF Student, CCSF Hong Yu 2004-2005 Staff Research Associate II,

UCSF Staff Research Associate II, UCSF

Michael Bingen 2004-2005 Staff Research Associate I, UCSF

Lead Engineer, Switchfly Inc, San Francisco, CA

Brian Wolff 2004-2005 Staff Research Associate I, UCSF

PhD Student, Georgetown, Washington DC

Linda Hicks 2004-2005 Staff Research Associate I, UCSF

Unknown

Mini Jan 2005-2006 Sr. Research Technologist, SJCRH

Associate Chemist, Dow AgroSciences

Alexander Arnold 2005-2009 Staff Scientist – SJCRH Associate Professor, University of Wisconsin, Milwaukee

Michele Connelly 2005-present Associate Scientist, SJCRH Associate Scientist, SJCRH Neena Joshi 2006-2007 Senior Research

Technologist, SJCRH Executive Lead Pharmacist, Target, Minneapolis MN

Cynthia Nelson 2006-2008 Research Technologist, SJCRH

Field Automation Engineer, Tecan, Memphis, TN

Aaron Kosinski 2006-2008 Research Technologist, SJCRH

Graduate Student in Bioengineering, University of Minnesota

Fangyi Zhu 2007-present Sr. Research Technologist, SJCRH

Research Scientist, QPS, Raleigh-Durham, NC

Cindy Choy 2007-2008 Research Technologist, SJCRH

Graduate Student, Washington State University

Min Lu 2007-2011 Sr. Research Technologist, SJCRH

Owner, PMA-Naperville, IL

Priya Velusamy 2008-2009 Sr. Research Technologist, SJCRH

Research Scientist, Alkem Laboratories, Kamataka, India

Jaeki Min 2009- present

Staff Scientist SJCRH Staff Scientist SJCRH

Julie Clark 2009- present

Sr. Research Technologist, SJCRH

Sr. Research Technologist, SJCRH

Dena (Hodges) Pavlicek

2009-2011 Sr. Research Technologist, SJCRH

Technical Services Chemist, Delta Foremost Chemical Corporation

Amy Orcutt 2011- present

Research Technologist, SJCRH

Regulatory Affairs Specialist, Wright Medical Technology, Memphis, TN

Gloria Holbrook 2011- present

Research Technologist, SJCRH

Product Development Manager, BASi, Charlotte NC

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Yandira Salinas 2011- present

Research Technologist, SJCRH

Graduate Student, UTHSC

Deepak Bhasin 2012- present

Sr. Research Technologist, SJCRH

Sr. Research Technologist, SJCRH

Postdoctoral Fellows: Name Years in

Lab Project Current Position

Thomas Robertson (CBCR Fellow)

1999-2001

Synthesis of Designed Inhibitors of Nuclear Receptor Function

Senior Bioanalytical Chemist, CPR Pharma, Adelaide, AUS

Prudencio Herradura 1999-2001

Total Synthesis of Phalloidin Global Regulatory Affairs Manager, Baxalta, Los

Angeles, CA Chris Collins

(UCSF Biochemistry Training Grant Fellow)

2000-2001

Synthesis of Novel Protein Crosslinking Reagents

Deceased

Naoaki Fujii (Visiting Scientist,

Fujisawa Pharmaceuticals)

2000-2001

Synthesis of Beta Strand Peptidomimetics

Associate Member of Chemical Biology and Therapeutics, SJCRH

Wenchen Luo 2001-2004

Synthesis of Designed Alpha Helical Peptidomimetic

Inhibitors of Nuclear Receptor Function

Director, Pharmacyclics, San Francisco, CA

Marc Anderson 2001-2005

Total Synthesis of Phalloidin Assistant Professor of Chemistry, San Francisco

State University A. “Leggy” Arnold 2002-

2005 Synthesis of Designed Alpha

Helical Peptidomimetics Associate Professor of

Chemistry, U Wisconsin Milwaukee

Chun Chow 2004-2005

Synthesis of Aspartyl Protease Inhibitors

Scientist II, Medicinal Chemistry, Mpex Pharmaceuticals

Helen Franks 2005 Synthesis of Inhibitors of the Interaction of HIV TAR with

TAT

Head of Chemistry and Production, Dextra

Laboratories Anang Shelat 2005-

2010 Visualization of High-

Throughput Data Assistant Member of

Chemical Biology and Therapeutics, SJCRH

Clementine Feau 2005-2009

Androgen Receptor/Transcriptional

Coregulator Interactions as Novel Targets in Prostate Cancer Drug Discovery

Research Scientist II, Broad Institute

David Lowes 2005- Parallel Synthesis of Anti- Lab-Assistant

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2012 malarial Therapeutics Based On Privileged Scaffolds

Oxford Immunotec

Armand Guiguemde 2006-2010

Identification Of Novel Antimalarials By Cell

Based High Throughput Screening

Staff Scientist, SJCRH

Jong Yeon Hwang 2006-2011

Discovery Of Thyroid Hormone Receptor (TR)-

Coactivator Inhibitors And Study Of Their Biological

Effect

Senior Researcher, Korea Institute of Chemical

Technology, Seoul KOR

Yiqun “Joyce” Zhang 2006-2011

Synthesis of WHO/TDR 17516 Analogues as

Antimalarials

Senior Chemist, Dow Chemical

Jennifer (Atkinson) Xavier (co-supervised with Dr. Gilbertson)

2006-2010

Repurposing for Ependymoma

Assistant Professor of Pediatrics, Penn State

Hershey, PA Prabodh Sadana 2007-

2009 Mechanism of Action of

Thyroid Hormone Receptor Coactivator Inhibitors

Assistant Professor, Northeastern Ohio Unified

College of Medicine Catherine Regni (co-supervised with Dr.

Schulman

2008-2009

Structure of MDMX with Bound Inhibitors

Validation Engineer, Sigma Aldrich

Ramy Attia 2009-2014

Regulation of Mitochondrial Respiration by Nuclear

Hormone Receptors

Home Infusion Clinical Pharmacist, BioScript,

Memphis, TN Praveen Kumar

Suryadevara 2010-2013

Synthesis of ATM Inhibitors Senior Research Scientist, Symmetry Biosciences

Erin Daly 2011-2013

Inhibitors of the interaction of the Androgen Receptor

and FKBP52

Technical Specialist, McCarter and English, LLP

Kristin Finch (co-supervised with Dr.

Dyer)

2011-2014

Inhibitors of the Interaction of p53 and MDMX

STEM Diversity Program Manager, Tufts University

Birgit Nimmervoll 2011-2015

Repurposing for Choroid Plexus Carcinoma

Principal Scientific Associate, Cancer Research

UK, Cambridge UK Eleanor Pritchard 2011-

present Slow-release Subconjunctival

Formulations for Drugs for Retinoblastoma

Postdoctoral Research Associate, SJCRH

David Barnett 2012- present

Lead optimization of the Diaminonapthoquinones

Postdoctoral Research Associate, SJCRH

Angela Carrillo 2013- present

Discovery of novel anti-trypanosomal drug leads

Postdoctoral Research Associate, SJCRH

Jared Hammill 2013- Optimization of DCN1, a Postdoctoral Research

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present novel target for epigenetic regulation of oncogenesis

Associate, SJCRH

Junior Faculty: Name Years Starting Position Current Position

Naoaki Fujii 2005- present

Assistant Member, Chemical Biology and Therapeutics,

SJCRH

Associate Member, Chemical Biology and Therapeutics,

SJCRH Taosheng Chen 2006-

present Assistant Member, Chemical

Biology and Therapeutics, SJCRH

Associate Member, Chemical Biology and Therapeutics,

SJCRH Michael Taylor 2009-

2015 Assistant Member, Chemical

Biology and Therapeutics, SJCRH

Assistant Professor, Pharmaceutical Sciences, University of Wisconsin,

Madison Fatima Rivas 2010-

present Research Associate,

Chemical Biology and Therapeutics, SJCRH

Assistant Member, Chemical Biology and Therapeutics,

SJCRH Anang Shelat 2011-

present Assistant Member, Chemical

Biology and Therapeutics, SJCRH

Assistant Member, Chemical Biology and Therapeutics,

SJCRH Tudor Moldoveanu 2014-

present Assistant Member, Chemical Biology and Therapeutics and

Structural Biology, SJCRH

Assistant Member, Chemical Biology and Therapeutics and

Structural Biology, SJCRH

PROFESSIONAL ACTIVITIES Service to Public Institutes, Societies, and Public Private Partnerships Prior: 1/03-10/06: Member, Steering Group on Genomics and Drug Discovery, Tropical Disease

Research Unit, World Health Organization 7/05-9/10: Member, Scientific Advisory Board, Medchem Program, National University of

Singapore 3/06: Member, NIH Advisory Committee on Compound Acquisition for the Roadmap 05/06-9/10: Member, PubChem Scientific Advisory Board 7/06-7/13: Member, Medicines for Malaria Venture Expert Scientific Advisory Committee 4/09-7/10: Chair, MMV Expert Scientific Advisory Committee Discovery Section 6/09: Member, University of North Carolina (UNC)-Chapel Hill Cancer Center, State

Funding External Advisory Board 1/12: Member, UK-Higuchi Biosciences Center Review Board 5/10-5/13: Member, Fellowship Advisory Committee Damon Runyon Foundation Current: 1/09-present: Member, Moffitt Cancer Center PO1 Scientific Advisory Board 6/13-present: Member, Board of Scientific Counselors, National Center for Biotechnology

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Information, National Library of Medicine 9/13-present: Member, Scientific Advisory Board, GSK Open Lab Foundation

Organization of Meetings Prior: 6/99: Organizer and Chair, Symposium on Chemical Biology, 54th Northwest Regional Meeting of the American Chemical Society 2/04: Organizer and Chair, CHI Library Design and Organic Synthesis Meeting, Target-

Oriented Synthesis Versus Diversity-Oriented Synthesis Section 5/04: Organizer and Chair, QB3 “High-Throughput High Return Studies for Biomedical

Sciences,” 7/04-7/06: Vice-Chair (2005) and Chair (2006) Gordon Research Conference on

Combinatorial 03/09: Organizer and Chair, Keystone Symposia – Protozoal Drug Discovery 04/09: Organizer and Chair, NIDDK/NIH – Chemical Approaches to Nuclear Receptors

and Metabolism 2/12: Chair, Molecular Approaches to Malaria – Drug Discovery Session 11/12: Session Chair, Genomic Approaches to Malaria, American Society of Tropical

Medicine and Hygiene Annual Meeting 1/13: Session Chair, 11th Winter Conference on Medicinal Chemistry Service to Industry Prior: 5/99-8/05: Due Diligence Consultant, Versant Venture Capital 8/00-8/07: Scientific Advisory Board (SAB) Orphagen Pharmaceuticals 8/01-8/04: SAB Genospectra, Inc. 2/04-5/06: SAB Zorphion Pharmaceuticals Current: 5/03–present: SAB Arbor Vitae 8/05-present: SAB Advanced Genetic Systems 8/05-present: SAB Biavolo Formal Study Sections Prior: 4/02-9/06: Member, NSF, Panel on Nanotechnology 5/02: Ad Hoc Member, NIH Bioorganic and Natural Products Chemistry Study Section 4/04-6/06: Member, NIH Special Emphasis Panel, Zebrafish Genetics and Screening Study

Section 5/05-8/10: Member, NIH Drug Discovery Special Emphasis Panel 9/05: Reviewer, NIH Road Map Program 6/06: Ad Hoc Member, NIH Nuclear Dynamics and Transport Study Section 10/06: Reviewer, NIH/Synthetic and Biological Chemistry (SBCA) Study Section

(NOT-OD-067) 11/06: Reviewer, NIH/Drug Development (ZRG1 MDCN-C 91S) 12/06: Reviewer, Cystic Fibrosis Grant Review

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5/08: Reviewer, NIH Special Emphasis Panel (RFA-RM-08-003) 1/09–5/13: Member, Damon Runyon Fellowship Award Committee 1/10: Ad Hoc Member, NIH/SBCA Study Section Current: 10/98-present: Reviewer, Austrian National Research Council, Molecular Genetics Subsection,

National Research Grants 5/00-present: Reviewer, Petroleum Research Fund, ACS 11/00-present: Reviewer, Austrian National Research Council Division of Lipid Biology,

National Research Grants 09/06-present: Reviewer, A*Star Program, Singapore 08/07-present: Reviewer, Swedish National Research Council 12/07-present: Reviewer, Linneus Foundation 2/08-present: Reviewer, Wellcome Trust 5/08-present: Regular Study Section Member, Walter Reed Army Institute of Research 7/12-6/18: Member, NIH Synthetic and Biological Chemistry B Study Section Service to Scholarly and Professional Journals Editorial Board Service 1/07-1/09: Editorial Advisory Board, Journal of Combinatorial Chemistry 2/09-present: Editorial Advisory Board, ACS Combinatorial Science 6/12-present: Board of Reviewing Editors, Science 7/14-present: Editorial Advisory Board, Journal of Medicinal Chemistry Reviewer Service 10/99-present: Reviewer, Bioorganic and Medicinal Chemistry Letters 7/01-present: Reviewer, Journal of Combinatorial Chemistry 6/02-present: Reviewer, Journal of the American Chemical Society 10/03-present: Reviewer, Journal of Organic Chemistry 2/04-present: Reviewer, Organic Letters 1/07-present: Reviewer, Nature Chemical Biology 1/07-present: Reviewer, ACS Chemical Biology 1/07-present: Reviewer, Journal of Medicinal Chemistry

UNIVERSITY AND HOSPITAL

St Jude Children’s Research Hospital Prior: 4/05-4/09: Faculty Appointments and Promotions Committee 4/05-2/06: Strategic Planning Committee 1/09-2/10: Pharmacokinetics Task Force 4/08-4/10: Institutional Biosafety Committee 1/10-3/10: Strategic Planning Committee 4/05-8/10: Institutional Biosafety Committee 12/09-7/11: Chair, Computational Biology Task Force 7/11-5/12: Nuclear Medicine Strategic Planning Committee

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10/06-6/14: Management Council Current: 4/05-present: Executive Committee 7/06-present: Cancer Center Advisory Board 9/06-present: Chair, Translational Resources Allocation Committee 4/10-present: Translational Therapeutics Candidate Committee 2/11-present: PK Shared Resource Oversight Committee 3/11-present: Drug Discovery Strategic Task Force 9/11-present: Search Committee, Chair of Computational Biology 9/11-present: Search Committee, Chair of Cancer Biology 6/14-present: Strategic Planning Committee Core Committee Basis Science Subcommittee Translational Science Subcommittee 10/14-present: Institutional Animal Care and Use Committee 10/15-present: Basic Science Council Thesis Committees – SJCRH 03/07–present: Asad Taherbhoy 12/07–5/11: Katie Nemeth 5/09–11/11: Fang Yan UCSF Service University-Wide 7/00-7/02: Alternate Delegate for UCSF, Academic Senate 4/04-9/05: UCSF Delegate to Regional Translational Research Planning Committee 8/04-9/05: Pharmastart Steering Committee Campus-Wide 9/98-9/00: UCSF Mission Bay Design, Chemistry User Group Section 7/99-11/99: Co-Organizer, Second Annual UCSF Chemistry and Cancer Meeting 3/00-6/01: Chancellor's Ad Hoc Committee for the Supportive Work Environment Initiative 6/00-9/05: UCSF Chemical Safety Committee 9/00-6/01: Chancellor’s Advisory Committee on Housing 12/00-9/05: Mission Bay Operations and Services Committee

- 12/00-present: Member, User’s Subcommittee - 6/01-present: Co-Chair, User’s Subcommittee - 9/01-present: Member, Core Planning Committee

12/00-9/05: Conflict of Interest Advisory Committee 10/02-9/05: UCSF Committee on the Library 1/03-9/05: Program in Population Sciences and Global Health, Education Subcommittee 9/03-9/05: Chair, UCSF Transportation Advisory Committee School of Pharmacy 9/00-8/01: School of Pharmacy Informatics/Library Committee

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9/01-9/05: School of Pharmacy Safety Committee

Department of Pharmaceutical Chemistry 9/98-6/99: Department of Pharmaceutical Chemistry Faculty Search 10/98-12/99: Department of Pharmaceutical Chemistry, Seminar Committee 10/01-9/05: Department of Pharmaceutical Chemistry Faculty Search

Graduate Program in Biological Sciences Qualifying Examinations 10/98: Member, Hikari Yoshihara, Program in Biological Sciences 3/00: Member, David Carroll, Program in Biological Sciences 5/01: Member, Jennifer Paulson, Program in Biological Sciences Graduate Program in Biophysics Qualifying Examinations 2/01: Chair, Zach Serber 3/01: Chair, Nilesh Shah Thesis Committees 2/01-7/03: Zach Serber 8/03-9/05: Eric Slika 12/03-12/09: Eugene Hur Graduate Program in CCB (Pharmaceutical Chemistry) 6/00-12/00: Retreat Committee, CCB Graduate Program 11/99-5/01: Admissions Committee, CCB Graduate Program 9/04-12/04: Retreat Committee, CCB Graduate Program Qualifying Examinations 2/00: Member, Tao Shi 5/00: Member, Giselle Knudsen 6/00: Member, Sami Mahrus 12/00: Chair, Ngoc-Ha Nguyen 3/01: Member, Nicola Clegg 3/01: Chair, Andrew Verras 6/01: Member, Natasja Brooijmans 8/01: Member, Steph Truhlar 11/01: Member, Kevin Masukawa 4/02: Member, Mike Gage 4/02: Member, Michael Cohen 5/02: Member, Zachary Knight 8/02: Member, Justin Blethrow 2/03: Member, Theresa Downing 4/03: Member, Edwin Tan 5/03: Member, Raynard Bateman 11/03: Member, Cory Ocasio

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Thesis Committees 6/00-6/04: Giselle Knudsen 3/01-4/05: Ha Nguyen 8/01-5/05: Nicola Clegg 10/1-9/05: Andrew Verras 12/01-3/05: Steph Truhlar 4/01-7/05: Kevin Masukawa 5/02-8/05: Michael Cohen 5/02-8/05: Alan Marnett 4/03-2/05: Mike Gage 4/03-9/05: Nathan Sallee 9/03-9/05: Theresa Downing 1/04-9/05: Cory Ocasio Graduate Program in Medical Information Sciences Qualifying Examinations 5/01: Member, Jose Haresco, Medical Information Sciences Thesis Committees 6/01-6/03: Jose Haresco, Medical Information Sciences Graduate Program in Biopharmaceutical Sciences Qualifying Examinations 11/01: Member, Valerie Ng, Program in Biological Sciences Thesis Committees 4/02-9/05: Member, Valerie Ng, Program in Biological Sciences Graduate Program in Quantitative Biology 2/01-5/01: Program in Quantitative Biology Curriculum Committee University of Vienna, Department of Biochemistry Thesis Committees 4/01-: Isabella Halama, (locally supervised by Peter Walters) Invited Lectures and Seminars 4/00: UCSF Cancer Center, “Alpha Helical Peptidomimetics” 10/00: UCSF Tetrad Graduate Program Symposium, “Alpha Helical Peptidomimetics” 11/00: UCSF Department of Anesthesia, “Alpha Helical Peptidomimetics” 11/00: UCSF/Harvard Symposium on Herbal Therapies and Dietary Supplements, “How does an herb become a drug? Taxol as a case study” 01/01: California State University Los Angeles, Department of Chemistry, “Alpha Helical Peptidomimetics” 02/01: Orphagen, Inc. “High Throughput Assay of Nuclear Hormone Receptor • Co-regulator Interactions”

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3/01: Karo Bio USA, “Inhibitors of Thyroid Hormone Receptor Transcriptional Activation Complex Formation” 3/01: UCSF Prostate Cancer Retreat, “Interrupting assembly of nuclear hormone receptor transcriptional activation complexes: Implications for drug development” 5/01: Twelfth World Molecular Engineering Network Conference, Cabo San Lucas, Mexico “Alpha Helical Peptidomimetics Targeting the Nuclear Receptor Coregulator Interface” 6/01: GenoSpectra, “Applications of Chemical Genomics” 7/01: Structural Genomix, “Inhibitors of Thyroid Hormone Receptor Transcriptional Activation Complex Formation” 9/01: Karo Bio, Sweden, “Inhibitors of Thyroid Hormone Receptor Transcriptional Activation Complex Formation” 9/01: ACS National Meeting, “Inhibitors of Thyroid Hormone Receptor Transcriptional Activation Complex Formation” 10/01: Plexxicon, “Systems Approaches to Signaling Research Using Chemical Inhibitors of Protein Interactions” 4/02: University of California Davis, Department of Chemistry, “Alpha Helical Proteomimetics” 5/02: San Diego State University, Department of Chemistry, “Alpha Helical Proteomimetics” 5/02: University of California Santa Barbara, Department of Chemistry, “Alpha Helical Proteomimetics” 4/02: San Diego State University, Department of Chemistry, “Alpha Helical Proteomimetics” 7/02: Gordon Conference in Combinatorial Chemistry, Oxford, England, “A Tale of Two Helicies” 7/02: International Union of Pure and Applied Chemistry Conference on Organic Chemistry, Christchurch New Zealand, “Application of Parallel Synthesis in the Production of Functional Alpha Helical Peptidomimetics” 7/02: Baker Medical Research Institute, Melbourne, Australia, Department of Cardiovascular Medicine, “The Inhibition of the Formation of Nuclear Hormone Receptor Transcriptional Activation Complexes Using Peptidomimetics”` 7/02: University of Queensland, Brisbane, Australia, Department of Chemistry, “Insights into Function of the Nuclear Hormone Receptor Transcriptional Activation Complex through Chemical Techniques” 7/02: University of Sydney, Sydney, Australia, Department of Chemistry, “Interrupting the Function of Signaling Regulatory Complexes with Peptidomimetics” 9/02: Stanford Research Institute, “Alpha Helical Peptidomimetics” 12/02: Banbury Conference, Cold Spring Harbor, “Functional Probes of Glucocorticoid Receptor” 1/03: The Scripps Research Institute, Department of Chemistry, “Chemical Proteomics Approaches to Understanding Regulation of Transcription by Nuclear Hormone Receptors” 3/03: Sandia National Laboratories, Livermore, CA, “Chemical Proteomics Approaches to Understanding Regulation of Transcription by Nuclear Hormone Receptors” 4/03: UCSF Professional and Academic Success Skills Seminar, “Writing, Publishing, and Creating Open Access to Scientific Literature” 4/03: Washington State University, Department of Chemistry, “Chemical Proteomics Approaches to Understanding Regulation of Transcription by Nuclear Hormone Receptors” 4/03: Arbor Vita Corporation, Redwood City, CA, “Chemical Approaches to Understanding and Regulating PDZ Domain Function”

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5/03: Roche Pharmaceuticals, Palo Alto, CA, “Chemical Proteomics Approaches to Understanding Regulation of Transcription by Nuclear Hormone Receptors” 5/03: Thirteenth World Molecular Engineering Network Conference, Cabo San Lucas, Mexico “Chemical Approaches to Regulating the PTEN, mdm2, p53 Tumor Suppressor Oncoprotein Network” 5/03: University of California Santa Cruz, Department of Chemistry, “Chemical Proteomics Approaches to Understanding Regulation of Transcription by Nuclear Hormone Receptors” 6/03: Gordon Research Conference on Hormones and Development, New London, CT “Chemical Proteomics Approaches to Understanding Transcriptional Activation by Nuclear Hormone Receptors” 6/03: Array Biopharma, Boulder, CO “The UCSF Cystic Fibrosis Drug Development Program” 6/03: UCSF Symposium on Entrepreneurship, “Walking the Tightrope: Balancing your Business and Academic Interests, Consultant Panel” 8/03: Gilead Pharmaceuticals, Foster City, CA “Chemical Approaches to Understanding and Regulating PDZ Domain Function” 8/03: Gilead Pharmaceuticals, Foster City, CA “HTS Cheminformatics” 9/03: University of Southampton, Southampton, England, “Chemical Proteomics Approaches to Understanding Regulation of Transcription by Nuclear Hormone Receptors” 9/03: Proteomic, Combinatorial, and Other Strategies for Drug Discovery, London, England, “Chemical Approaches to Understanding and Regulating PDZ Domain Function” 10/03: UCSF Cardiovascular Research Institute Retreat, “Inhibitors of PDZ Domain Function” 10/03: NSF Symposium on Collaborations in Chemistry, Washington, DC “MS3D – Moderate Resolution Protein Structures by Chemical Crosslinking, Mass Spectrometry, and Computation” 11/03: SJCRH, Memphis, TN “Inhibitors of PDZ Domain Protein Interactions” 12/03: CCB and Biophysics Joint Retreat, “Heterocycle Libraries as Lead Discovery Tools for Malaria” 2/04: IBM – Alamaden Research Institute, San Jose, CA “Chemical Proteomics Approaches to Understanding Nuclear Hormone Receptor Signaling” 2/04: CHI Library Design and Organic Synthesis, San Diego, CA, “Target Oriented Synthesis of Heterocycles - Microwaves, Parallel Purification, and Design” 5/04: AstraZeneca, Wilmington DE, “Chemical Proteomics Approaches to Understanding Nuclear Hormone Receptor Signaling” 6/04: University of Washington, Seattle WA, “Drug Discovery for Malaria” 7/04: Myriad Pharmaceuticals, Salt Lake City, UT, “Inhibitors of PDZ Domain Protein Interactions” 8/04: Gordon Conference in Combinatorial Chemistry, Oxford, England, “Lead Discovery and Optimization for Antimalarials” 9/04: UCSF Tetrad Retreat, Lake Tahoe, CA, ”Targeting Neglected Diseases” 9/04: Trypanosome Drug Development, Seattle, WA, “Compound Validation for Trypanosomal Disease Therapeutics” 11/04: Vanderbilt University, Nashville, TN. “Lead Discovery and Optimization for Antimalarials” 1/05: University of California Irvine, Irvine, CA, “Screening and Synthesis for Antimalarials” 2/05: Lawrence Livermore National Laboratories, Livermore, CA, “Designed Generic Libraries – Rapid Lead Discovery for Orphan Diseases” 3/05: Goteborg University, Goteborg Sweden, “Library Design for Academic Screening

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Facilities” 4/05: Keystone Symposium on Drugs against Protozoal Parasites, Copper Mountain, CO “Lead Discovery for Malaria” 5/05: Society for Biomolecular Screening, Redwood City, CA, “Screening and Synthesis for Antimalarials” 7/05: Bay Area Parasite Consortium, San Francisco, CA, “Screening and Synthesis for Antimalarials” 9/05: Vanderbilt University, Nashville, TN, “Lead Discovery for Malaria” 10/05: Buck Institute, Novato, CA, “Chemical Proteomics of Nuclear Hormone Receptors,” 5/06: International Symposium on Chemistry, Biology, and Medicine, Paphos, Cyprus, “Regulation of the Assembly of the Thyroid Receptor Transcriptional Regulatory Complex” 6/06: Gordon Research Conference on Host-Parasite Biology, Newport, RI, “Lead Discovery for Malaria” 6/06: Conference on Drug Discovery for AIDS, Bethesda, MD “Inhibition of the Interaction of HIV-Rev Protein and the Rev Response Element” 7/06: Biology of the Parasite Short Course, Woods Hole, MA., “Discovery and Development of New Drugs for Parasitic Diseases” 8/06: University of Southampton, England “Novel Inhibitor of Thyroid Hormone Signaling” 8/06: University of Goteborg, Sweden “Novel Inhibitor of Thyroid Hormone Signaling” 2/07: ACS, Chemistry in Cancer Research: A Vital Partnership, San Diego, CA, “A Novel Inhibitor of Androgen Receptor Function” 2/07: CERN: Ependymoma Symposium, Cancun Mexico, “Screening for Inhibitors of Ependymoma Oncogenesis” 2/07: Medicinal Chemistry and Molecular Pharmacology Seminar Series, Purdue University, Lafayette, IN, “The Chemical Proteomics of Nuclear Hormone Receptors” 3/07: The Kimmel Scholars’ Symposium, Palm Beach, FL, “A Novel Inhibitor of Thyroid Hormone Function” 3/07: Carlsberg Laboratory Friday Lectures, Copenhagen, Denmark, “Screening and Synthesis for Novel Antimalarials” 4/07: Reed College, Portland, OR, “Screening and Synthesis for Novel Antimalarials” 4/07: Oregon Health & Science University, Portland, OR, “Screening and Synthesis for Novel Antimalarials” 7/07: Biology of Parasitism Modern Approaches: Marine Biological Laboratory, Woods Hole, MA, “Development of Antiparasitic Drugs” 8/07: Vanderbilt Institute of Chemical Biology, Nashville, TN, “Drug Discovery: Assay to Probe” 8/07: ACADIA Pharmaceuticals, Malmo Sweden, “Discovery of Novel Antimalarials” 9/07: University of Arkansas, Fayetteville, AR, “Screening and Synthesis for Novel Antimalarials” 11/07: Institute for Translational Medicine and Therapeutics, Philadelphia, PA, “Novel Antimalarials” 2/08: University of Minnesota Department of Medicinal Chemistry, Minneapolis, MN, Screening and Synthesis for Novel Antimalarials” 3/08: University of Pittsburgh, Pittsburgh, PA, “New Approaches to Antitrypanosomal Drugs” 3/08: Expert Drug Discovery Advisory Committee Meeting, Geneva, Switzerland, “TDR 17516 Project for Malaria (Project Review)”

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4/08: National ACS Meeting, Medicinal Chemistry Symposium, “Novel Inhibitors of Thyroid Hormone Function” 5/08: Walter Reed Army Institute for Research (WRAIR), “Discovery of Antimalarials” and “Discovery of Antitrypanosomals,” 5/08: UNC-Chapel Hill Annual Drug Discovery Symposium “Novel Inhibitors of Thyroid Function” 5/08: WRAIR, Bethesda, MD “Screening and Synthesis for Novel Antimalarials” 5/08: WRAIR, Bethesda, MD “Screening and Synthesis for Novel Antitrypanosomals” 6/08: Gordon Research Conference on Bioorganic Chemistry, Andover, MA, “A Novel Inhibitor of Thyroid Hormone Function” 9/08: Biology of Parasitism Modern Approaches: Marine Biological Laboratory, Woods Hole, MA, “Discovery and Development of Antiparasitic Drugs” 11/08: University of Tennessee Health Sciences Center, Department of Physiology “A Novel Inhibitor of Thyroid Hormone Function” 1/09: Moffitt Cancer Center, Tampa, FL, “A Novel Inhibitor of Thyroid Hormone Function” 2/09: Molecular Diversity in Chemical Biology and Drug Discovery: New York Academy of Sciences, New York, NY “A Novel Inhibitor of Thyroid Hormone Function ” 03/09: 10th Drug Design & Development Seminar: Justus-Liebig-Universitä, Giessen Germany, “Screening and Synthesis for Novel Antimalarials” 03/09: Keystone Symposium on Drug Discovery for Protozoan Parasites, Breckenridge, CO “Early Lead Optimization for a Novel Series of Antimalarials” 5/09: DMPK Chemistry Workshop, Capetown, South Africa, “Practical Path to First Time In Animals” 7/09: Biology of Parasitism Modern Approaches: Marine Biological Laboratory, Woods Hole, MA, “Discovery and Development of Antiparasitic Drugs” 8/09: 10th Annual Symposium in Functional Genomics, Goteborg, Sweden, “An Inhibitor of the Function of the Thyroid Hormone Receptor” 1/10: Memorial Sloan Kettering Cancer Center, New York, NY “A Novel Inhibitor of the Interaction of p53 and MDMX,” 3/10: Texas A&M, College Station, TX, “Screening for Novel Antimalarials” 7/10: UCSF, San Francisco, CA “Screening and Synthesis for Novel Antimalarials” 9/10: European Laboratory Robotics Interest Group, Coventry, England “Discovery of Novel Antimalarials” 9/10: Georgetown University, Washington DC, “Screening for Antimalarials” 1/11: University of Alabama, “Discovery and Development of Novel Antimalarials” 2/11: Roche Chemistry Frontiers, Basel, Switzerland “Development of Inhibitors of the Interaction of the Thyroid Hormone Receptor and its Obligate Cofactors” 3/11: Dunne Lecture, Reed College, Portland Oregon “Development of Antimalarials” 3/11: Society for Biomolecular Screening Annual Meeting, “Phenotypic Screening to Identify New Leads for Malaria” 4/11: Walter Reed Army Institute of Research, Bethesda, MD “Development of Novel Antimalarials Based on Phenotypic Screening Hits,” 5/11: University of Kansas, Lawrence, KS “Inhibitors of the Thyroid Hormone Receptor Interaction with Coactivators” 5/11: Montana State University, Bozeman, MT “Discovery and Development of Antimalarials” 6/11: Polyamine Gordon Research Conference, Manchester, NH “Discovery of Novel Inhibitors

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of Ornithine Decarboxylase for Sleeping Sickness” 8/11: ASMC Conference, St Petersburg, Russia, “Development of the Dihydroisoquinolines, Orally Available Antimalarials” 9/11: MPM Meeting, Woods Hole, MA “Development of the Dihydroisoquinolines, Orally Available Antimalarials” 1/12: Broad Institute, Cambridge, MA “Phenotypic Screening to Find New Leads for Drug Development” 3/12: Keystone Symposium – Addressing the Challenges of Drug Discovery, “Development of the Dihydroisoquinolines, Orally Available Antimalarials” 4/12: University of South Florida, Tampa, FL “Development of the DHIQ’s as Novel Orally Bioavailable Antimalarials” 5/12: University of Notre Dame, Notre Dame, IN “Development of Novel Antimalarials” 6/12: Harvard Medical School, Cambridge, MA, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 6/12: Boston University, Boston, MA, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 9/12: Indiana University, Indianapolis, IN “Discovery and Development of Novel Antimalarials,” 10/12: H3-D Symposium, Cape Town, South Africa, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 11/12: ACS Regional Meeting, Baton Rouge LA, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 2/13: American Association for the Advancement of Science National Meeting, “Phenotypic Approaches to Lead Discovery” 3/13: NIDDK Symposium on Chemical Biology, “Discovery of Novel Classes of Thyroid Antagonists,” 4/13: Vanderbilt University, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 5/13: Tennessee Technological University, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 5/13: University of Minnesota, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 6/13: Seattle Biomedical Research Institute, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 9/13: Louisiana State University, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 9/13: Tulane University, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 10/13: 1st Symposium on Frontier Sciences on new Drug Discovery, Beijing, China, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 10/13: Scripps Research Institute, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 1/14: University of Georgia, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 2/14: Union University, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials”

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4/14: University of Washington, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 6/14: Gordon Conference on Host-Parasite Interactions, Newport, RI, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 11/14: Washington University, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 8/15: U Southern Mississippi, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 9/15: Michigan State University, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials” 9/15: London School of Tropical Medicine, “Development of the DHIQs as Novel Orally Bioavailable Antimalarials”

Bibliography

Journal Articles Papers from work at IBM (Industrial Technician) 1. Guy, R. K.; DiPietro, R. A. “A Facile One-Pot Synthesis of Symmetrical and Unsymmetrical

Acetaldehyde Acetals from Primary Alcohols,” Synth. Commun. 1992, 22, 687-692. 2. Ito, H.; Dalby, C.; Pomerantz, A.; Sherwood, M.; Sato, R.; Sooriyakumaran, R.; Guy, K.;

Breyta, G. “Monomer Reactivities and Kinetics in Radical Copolymerization of Hydroxystyrene Derivatives and tert-Butyl (Meth)acrylate,” Macromol. 2000, 33, 5080.

Papers from Nicolaou Laboratory (Graduate School) 1. Nicolaou, K. C.; Liu, J. J.; Hwang, C. -K.; Dai, W. -M.; Guy, R. K. “Synthesis of a Fully

Functionalized CD Ring System of Taxol,” J. Chem. Soc. Chem. Commun. 1992, 1118-1120. 2. Nicolaou, K. C.; Dai, W. -M.; Guy, R. K. “The Chemistry and Biology of Taxol,” Angew.

Chem. Int. Ed. Engl. 1994, 33, 15-44. 3. Nicolaou, K. C.; Nantermet, P. G.; Ueno, H.; Guy, R. K. “Retrosynthetic and Synthetic

Studies towards the Synthesis of Taxol,” J. Chem. Soc. Chem. Commun. 1994, 295-296. 4. Nicolaou, K. C.; Yang, Z.; Liu, J. J.; Ueno, H.; Nantermet, P. G.; Guy, R. K.; Claiborne, C.

F.; Renaud, J.; Couladouros, E. A.; Paulvannan, K.; Sorensen, E. J. “Total Synthesis of Taxol,” Nature, 1994, 367, 630-634.

5. Nicolaou, K. C.; Guy, R. K.; Wrasidlo, W.; Pitsinos, E. “A Water-Soluble Prodrug of Taxol with Self-Assembling Properties,” Angew. Chem. Int. Ed. Engl. 1994, 33, 1583-1587.

6. Nicolaou, K. C.; Couladouros, E. A.; Nantermet, P. G.; Renaud, J.; Guy, R. K. “Synthesis of C-2 Taxol Analogs,” Angew. Chem. Int. Ed. Engl. 1994, 33, 1581-1583.

7. Paloma, L. G.; Guy, R. K.; Wrasidlo, W.; Nicolaou, K. C. "Conformation of a Water-Soluble Derivative of Taxol in Water by 2D-NMR Spectroscopy," Chem. Biol. 1994, 1, 107-112.

8. Nicolaou, K. C.; Nantermet, P. G.; Ueno, H.; Guy, R. K.; Couladouros, E. A.; Sorensen, E. J. "Total Synthesis of Taxol. 1. Retrosynthesis, Degradation, and Reconstitution," J. Am. Chem.

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Soc. 1995, 117, 624-633. 9. Nicolaou, K. C.; Liu, J. -J.; Yang, Z.; Ueno, H.; Sorensen, E. J.; Claiborne, C. F.; Guy, R. K.;

Hwang, C. -K.; Nakada, M.; Nantermet, P. G. "Total Synthesis of Taxol. 2. Construction of A and C Ring Intermediates and Initial Attempts to Construct the ABC Ring System," J. Am. Chem. Soc. 1995, 117, 634-644.

10. Nicolaou, K. C.; Yang, Z.; Liu, J. -J; Nantermet, P. G.; Claiborne, C. F.; Renaud, J.; Guy, R. K.; Shibayama, K. "Total Synthesis of Taxol. 3. Formation of Taxol's ABC Ring Skeleton," J. Am. Chem. Soc. 1995, 117, 645-652.

11. Nicolaou, K. C.; Renaud, J.; Nantermet, P. G.; Couladouros, E. A.; Guy, R. K.; Wrasidlo, W. "Synthesis and Biological Testing of C2-Taxol Derivatives," J. Am. Chem. Soc. 1995, 117, 2409-2420.

12. Nicolaou, K. C.; Guy, R. K. “The Conquest of Taxol,” Angew. Chem. Int. Ed. Engl. 1995, 34, 2079-2090.

13. Johnson, C. A.; Xu, Y.; Nicolaou, K. C.; Yang, Z.; Guy, R. K.; Dong, J. G.; Berova, N. “Enzymatic Resolution of a Key Stereochemical Intermediate for the Synthesis of (-) Taxol,” Tet. Lett. 1995, 36, 3291-3294.

14. Nicolaou, K. C.; Guy, R. K, Potier, P. “Taxoids: New Weapons Against Cancer,” Sci. Amer. 1996, 274, 94-99.

15. Guy, R. K.; Scott, Z. A., Sloboda, R. D.; Nicolaou, K. C. “Fluorescent taxoids,” Chem. Biol. 1996, 3, 1021-1031.

16. Nicolaou, K. C.; Claiborne, C. F.; Paulvannan, K.; Postema, M. H. D.; Guy, R. K. “The Chemical Synthesis of C-Ring Aryl Taxoids," Chem. Eur. J. 1997, 1, 399-409.

17. Nicolaou, K. C.; Guy, R. K.; Gunzner, J. L. “Intelligent Drug Discovery from Nature,” Medchem News, 1997, 3, 12-18.

18. Wrasidlo, W.; Gaedicke, G.; Guy, R. K.; Renaud, J.; Pitsinos, E.; Nicolaou, K. C.; Reisfeld, R. A.; Lode, H. N. "A novel 2'-(N-methylpyridiniumacetate) prodrug of Paclitaxel induces superior antitumor responses in preclinical cancer models," Biocon. Chem. 2002, 13, 1093-9.

Papers from Brown and Goldstein Laboratory (Postdoctoral Fellowship) 1. Dobrosotskaya, I.; Guy, R. K.; James, G. L. “MAGI-1: A Membrane-Associated Guanylate

Kinase with a Unique Arrangement of Protein-Protein Interaction Domains,” J. Biol. Chem. 1997, 272, 31589-31597.

2. Guy, R. K. “Inhibition of Sonic Hedgehog Autoprocessing in Cultured Mammalian Cells by Sterol Deprivation,” Proc. Natl. Acad Sci. 2000, 97, 7307.

Papers from Guy Laboratory (UCSF) 1. Herradura, P. S.; Pendola, K. A.; Guy, R. K. "Copper-Mediated Cross-Coupling of Aryl

Boronic Acids and Alkyl Thiols," Org. Lett. 2000, 2, 2019-22. 2. Geistlinger, T. R.; Guy, R. K. "An inhibitor of the interaction of thyroid hormone receptor

beta and glucocorticoid interacting protein 1," J. Am. Chem. Soc. 2001, 123, 1525-6.

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3. Novak, K.; Fujii, N.; Guy, R. K. "Investigation of the PDZ domain ligand binding site using chemically modified peptides," Bioorg. Med. Chem. Lett. 2002, 12, 2471.

4. Harris, B. Z.; Lau, F. W.; Fujii, N.; Guy, R. K.; Lim, W. A. “Role of Electrostatic Interactions in PDZ Domain Ligand Recognition,” Biochemistry, 2003, 42, 2797-2805.

5. Geistlinger, T. R.; Guy, R. K. “Novel Selective Inhibitors of the Interaction of Individual Nuclear Hormone Receptors with a Mutually Shared Steroid Receptor Coactivator 2,” J. Am. Chem. Soc. 2003, 125, 6852-6853

6. Springsteel, M. F; Galietta, L. J. V.; Ma, T.; By, K.; Berger, G. O.; Yang, H.; Dicus, C. W.; Choung, W.; Quan, C.; Shelat, A. A.; Guy, R. K.; Verkman, A. S.; Kurth, M. J.; Nantz, M. H. “Benzoflavone Activators of the Cystic Fibrosis Transmembrane Conductance Regulator: A Pharmacophore Model of Flavone-CFTR Binding,” Bioorg. Med. Chem. 2003, 11, 4113-4120.

7. Yang, H; Shelat, A. A.; Guy, R. K.; Gopinath, V. S.; Ma, T.; Du, K.; Lukacs, G. L.; Taddei, A.; Folli, C.; Pedemonte, N.; Galietta, L. J. V.; Verkman, A. S. “Nanomolar Affinity Small-Molecule Correctors of Defective dF508-CFTR Chloride Channel Gating,” J. Biol. Chem. 2003, 278, 35079-35085.

8. Fujii, N.; Haresco, J. J.; Pendola-Novak, K. A.; Stokoe, D.; Kuntz, I. D.; Guy, R. K., “A Selective Irreversible Inhibitor Targeting a PDZ Protein Interaction Domain,” J. Am. Chem. Soc. 2003, 125, 12074-12075.

9. Gochin, M.; Guy, R. K.; Case, M.; “A metallo-peptide assembly in fluorescence detection of ligand binding to the HIV-1 gp41 coiled coil,” Angew. Chem. Int. Ed. Engl. 2003, 5325-5328

10. Collins, C; Schilling, B.; Young, M.; Dollinger, G.; Guy, R. K. “Isotopically Labeled Crosslinking Reagents: Resolution of Mass Degeneracy in the Identification of Crosslinked Peptides,” Bioorg. Med. Chem. Lett. 2003, 13, 4023-4026.

11. Fujii, N.; Jacobsen, R. B.; Wood, N. L.; Schoeniger, J. S.; Guy, R. K. “A Novel Protein Crosslinking Reagent for the Determination of Moderate Resolution Protein Structures by Mass Spectrometry (MS3D),” Bioorg Med Chem Lett. 2004, 14, 427-429.

12. Geistlinger, T. L.; McReynolds, A.; Guy, R. K. “Ligand Selective Inhibition of the Interaction of Steroid Receptor Coactivators and the Estrogen Receptor,” Chem. Biol. 2004, 11, 273-281.

13. Evans, W. E.; Guy, R. K. “Gene Expression as a Drug Discovery Tool,” Nature Genetics, 2004, 36, 214-215.

14. Madrid, P. B.; Wilson, N.; DeRisi, J. L.; Guy, R. K., “Parallel Synthesis and Antimalarial Screening of a 4-Aminoquinoline Library,” J. Comb. Chem. 2004, 6(3), 437-442.

15. Moore, J. M. R.; Galicia, S. L.; McReynolds, A.; Ha, N. G.; Scanlan, T. S.; Guy, R. K. “Quantitative Proteomics of the Thyroid Hormone Receptor Coactivator Interaction,” J. Biol. Chem. 2004, 279(26), 27584-27590.

16. Arnold, A.; Luo, W.; Guy, R. K. “Synthesis of Medium Ring Heterocycles using an Intramolecular Heck Reaction,” Org. Lett. 2004, 6(17), 3005-3007.

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17. Anderson, M.; Moser, J.; Sherrill, J.; Guy, R. K., “A Convenient Procedure for Hydrolysis of Esters in Parallel Syntheses,” Synlett 2004, 2391-2399.

18. Fujii, N. Mallari, J. P.; Hansell, E. J.; Mackey, Z.; Doyle, P.; Zhou, Y. M.; Rosenthal, P. J.; McKerrow, J. H.; Guy, R. K. “Discovery of Potent Thiosemicarbazone Inhibitors of Rhodesain and Cruzain,” Bioorg Med. Chem. Lett. 2004, 15(1), 121-123.

19. Estébanez-Perpiñá, E.; Moore, J. M. R.; Mar, E.; Nguyen, P.; Delgado-Rodrigues, E.; Baxter, J.; Buehrer, B. M.; Webb, P.; Fletterick, R. J.; Guy, R. K. “The Mechanism of Ligand Dependent Transactivation by the Androgen Receptor”, J. Biol. Chem. 2005, 280, 8060-8.

20. Krylova, I. N.; Sablin, E. P.; Williams, J. D.; Williams, S. P.; Moore, J. M. R.; Xu, R. X. Waitt, G. M.; Juzumiene, D.; Bynum, J. M.; Montana, V.; Guy, R. K.; Thornton, J. W.; Fletterick, R. J.; Willson, T. M.; Ingraham, H. A. “Structural analyses of NR5 orphan receptors reveal a potential role as nuclear phospholipid sensors,” Cell, 2005, 120, 343-55.

21. Madrid, P. B.; Liou, A. L.; Sherrill, J.; Weisman, J.; DeRisi, J. L.; Guy, R. K. “Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities,” Bioorg Med. Chem. Lett. 2005, 15, 1015-8.

22. Anderson, M. A.; Shelat, A. S.; Moser, J.; Guy, R. K. “A Novel Solid-phase Approach to the Phallotoxins: Total Synthesis of [Ala7]-Phalloidin,” J.Org.Chem., 2005, 70, 4578-4584

23. Feng, B. Y.; Shelat, A. A.; Doman, T. N.; Guy, R. K.; Shoichet, B. K. “High-Throughput Assays for Promiscuous Inhibitors.” Nature Chemical Biology., 2005, 1, 146-148.

24. Anderson, M. O.; Sherrill, J.; Madrid, P. B.; Liou, A. P.; Weisman, J. L.; Derisi, J. L.; and Guy, R. K., "Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum," Bioorg Med Chem, 2006. 14(2): 334-43.

Papers from Guy Laboratory (SJCRH)

1. Arnold, L. A.; Estebanez-Perpina, E.; Togashi, M.; Jouravel, N.; Shelat, A.; McReynolds, A. C.; Mar, E.; Nguyen, P.; Baxter, J. D.; Fletterick, R. J.; Webb, P.; and Guy, R. K., "Discovery of small molecule inhibitors of the interaction of thyroid hormone receptor with transcriptional coregulators," J Biol Chem, 2005. 280(52), 43048-55.

2. Lu, F; Chi, S. W.; Kim, D. H.; Han, K. H.; Kuntz, I. D.; Guy, R. K. “Proteomimetic libraries: design, synthesis, and evaluation of p53-mdm2 inhibitors,” J. Combi. Chem., 2006, 8(3), 315-325.

3. Mills, N. L.; Daugherty, M. D.; Frankel, A. D.; Guy, R. K. “An a-helical inhibitor of the HIV-1 Rev-RRE Interaction,” J. Am. Chem. Soc., 2006, 128(11), 3496-7

4. Mackey, Z. B.; Baca, A. M.; Fujii, N.; Apsel, B.; Shelat, A.; Hansell, E. J.; Chiang, P. K.; Wolff, B.; Guy, R. K.; Williams, J.; McKerrow, J. “Discovery of trypanocidal compounds by whole cell HTS of live Trypanosoma brucei,” Chem. Biol. Drug. Des., 2006, 67(5), 355-367.

5. Madrid, P. B.; Liou, A. L.; DeRisi, J. L.; Guy, R. K. “Incorporation of an Intramolecular Hydrogen-bonding Motif in the Side-Chain of 4-Aminoquinolines Enhances Activity against Drug-Resistant P. falciparum.” J. Med. Chem. 2006, 49(15), 4535-4543.

6. May, B. C. H.; Witkop, J.; Sherrill, J.; Anderson, M. O.; Madrid, P. B.; Zorn, J. A.; Prusiner, S. B.; Cohen, F. E.; Guy, R. K, “Structure–activity Relationship Study of 9-Aminoacridine

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Compounds in Scrapie-Infected Neuroblastoma Cells,” Bioorg. Med. Chem. Lett. 2006, 16(18), 4913-4916.

7. Arnold, A.; Estébanez-Perpiñá, E; Togashi, M.; Shelat, A.; Ocasio, C. A.; McReynolds, A. C.; Nguyen, P.; Baxter, J. D.; Fletterick, R. J.; Webb, P.; Guy, R. K. “A High-Throughput Screening Method to Identify Small Molecule Inhibitors of Thyroid Hormone Receptor Coactivator Binding,” Sci. STKE, 2006, pl3.

8. Weisman, J. L.; Liou, A. P.; Shelat, A. A.; Cohen, F. E.; Guy, R. K; DeRisi, J. L. “Searching for New Antimalarial Therapeutics amongst Known Drugs,” Chem. Biol. Drug. Des., 2006, 67(5), 409-416.

9. Arnold, A.; Guy, R. K. “Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors,” Bioorg. Med. Chem. Lett. 2006, 16(20), 5360-5363.

10. Mayer, M.; Lang, P. T.; Gerber, S.; Madrid, P. B.; Gomez-Pinto, I.; Guy, R. K.; James, T. L. “Synthesis and Testing of a Focused Phenothiazine Library for Binding to HIV-1 TAR RNA,” Chem. Biol. 2006, 13(9), 993-1000.

11. Anderson, M. O.; Yu, H.; Penaranda, C.; Maddux, B. A.; Goldfine, I. D.; Youngren, J. F.; Guy, R. K. “Parallel Synthesis of Diarylureas and their Evaluation as Inhibitors of Insulin-Like Growth Factor Receptor,” J. Comb. Chem., 2006, 8(5), 784-90.

12. Fujii, N.; Haresco, J. J.; Novak, K. A. P.; Gage, R. M.; Pedemonte, N.; Stokoe, D.; Kuntz, I.

D.; Guy, R. K. “Rational Design of a Nonpeptide General Chemical Scaffold for Reversible Inhibition of PDZ Domain Interactions,” Bioorg. Med. Chem. Lett. 2006, 17(2), 549-552.

13. Fujii, N.; Shelat, A.; Hall, R. A.; Guy, R. K. “Design of a Selective Chemical Probe for Class I PDZ Domains,” Bioorg. Med. Chem. Lett. 2006, 17(2), 546-548.

14. Laurie, N. A.; Donovan, S. L; Shih, C.-S.; Zhang, J.; Mills, N.; Fuller, C.; Teunisse, A.; Lam, S.; Ramos, Y.; Mohan, A.; Johnson, D.; Wilson, M.; Rodriguez-Galindo, C.; Quarto, M.; Francoz, S.; Mendrysa, S. M.; Guy, R. K.; Marine, J.-C.; Jochemsen, A. G.; Dyer, M. A. “Inactivation of the p53 Pathway in Retinoblastoma,” Nature, 2006, 444(7115), 66-69.

15. Fujii, N.; You, L.; Xu, Z.; Uematsu, K.; Shan, J.; He, B.; Mikami, I.; Edmondson, L. R.; Neale, G.; Zheng, J.; Guy, R. K.; Jablons, D. M. “An Antagonist of Dishevelled Protein-Protein Interaction Suppresses b-catenin Dependent Tumor Cell Growth,” Cancer Research, 2007, 67(2), 573-579.

16. Warhust, D. C.; Craig, J. C.; Adagu, I. S.; Guy, R. K.; Madrid, P. B.; Fivelman, Q. L. “Activity of Piperaquine and other 4-aminoquinoline Antiplasmodial Drugs against Chloroquine-sensitive and Resistant Blood-stages of Plasmodium Falciparum. Role of beta-haematin inhibition and drug concentration in vacuolar water- and liquid-phases,” Biochem. Pharmacol. 2007, 73(12), 1910-1926.

17. Inglese, J.; Shamu, C. E.; Guy, R. K. “Reporting Data from High Throughput Screening of Small Molecule Libraries,” Nat. Chem. Biol. 2007, 3(8) 438-441.

18. Shelat, A.; Guy, R. K. “The Interdependence between Screening Methods and Screening Libraries,” Curr. Op. Chem. Biol. 2007, 11(3), 244-251.

19. Shelat, A.; Guy, R. K. “The Role of Scaffolds in Defining Functional Diversity of Screening

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Collections in Biologically Relevant Space,” Nat. Chem. Biol. 2007, 3(8), 442-446. 20. Mills, N. L.; Shelat, A. A.; Guy, R. K. “Assay Optimization and Screening of RNA:Protein

Interactions by Alphascreen,” J. Biomol. Screen. 2007, 12(7), 946-955. 21. Guy, R. K. “Cures for Neglected Diseases: Alternative Strategies for Finding Drugs,” Curr.

Op. Chem. Biol. 2007, 11(4), 10-11. 22. Hyatt, J. L.; Wadkins, R. M.; Tsurkan, L.; Hicks, L. D.; Hatfield, M. J.; Edwards, C. C.;

Ross, C. R.; Cantalupo, S. A.; Crundwell, G.; Guy, R. K.; Potter, P. M. “Planarity and Constraint of the Carbonyl Groups in 1,2-diones are Determinants for Selective Inhibition of Human Carboxylesterase 1,” J. Med. Chem., 2007, 50(23), 5727-5734.

23. Estebanez-Perpina, E.; Arnold, A. Webb, P.; Nguyen, P.; Delgado-Rodrigues, E.; Mar, E.; Bateman, R.; Pallai, P.; Shokat, K. M.; Baxter, J. D.; Guy, R. K.; Fletterick, R. J.; “A surface on the androgen receptor that allosterically regulates coactivator binding.,” Proc. Natl. Acad. Sci. USA, 2007, 104(41), 16074-16079.

24. Estebanez-Perpina, E.; Jouravel, N.; Arnold, A.; Togashi, M.; Blethrow, J.; Mar, E.; Nguyen, P.; Baxter, J. D.; Webb, P.; Guy, R. K.; Fletterick, R. J. “Structural Insight into the Mode of Action of a Direct Inhibitor of Thyroid Hormone Receptor Coregulator Binding,” Mol. Endocrin., 2007, 21(12), 2919-2928.

25. Mallari, J. P.; Shelat, A. A.; O’Brien, T.; Caffrey, C. R.’ Kosinski, A.; Connelly, M.; McKerrow, J. H.; Guy, R. K. “Development of Potent Purine-Derived Nitrile Inhibitors of the Trypanosomal Protease TbCatB,” J. Med. Chem. 2008, 51(3), 545-52.

26. Jouravel, N.; Sablin, E.; Arnold, L. A.; Guy, R. K.; Fletterick, R. J. “Interaction between the Androgen Receptor and a Segment of its Corepressor SHP,” Acta Cryst. 2007, D63, 1198-1200.

27. Arnold, A.; Kosinski, A.; Estebanez-Perpina, E; Fletterick, R. J.; Guy, R. K.; “Inhibitors of the Interaction of Thyroid Hormone Receptor and Coactivators: Preliminary Structure Activity Relationships,” J. Med. Chem. 2007, 50(22), 5269-5280.

28. Jouravel, N.; Sablin, E.; Arnold, L. A.; Guy, R. K.; Fletterick, R. J. “Interaction between the Androgen Receptor and a Segment of its Corepressor SHP,” Acta Cryst. 2007, D63, 1198-1200.

29. Guo, X.; Bandyopadhyay, P.; Schilling, B.; Young, M. M.; Fujii, N.; Aynechi, T.; Guy, R. K.; Kuntz, I. D.; Gibson, B. W. “Partial Acetylation of Lysine Residues Improves Intra-Protein Cross-linking,” Anal. Chem., 2008, 80(4), 951-60.

30. Shelat, A. A.; Guy, R. K. “A Road Less Traveled by: Exploring a Decade of Ellman Chemistry,” Bioorg. Med. Chem. 2009, 17(3), 1089-1093.

31. Mallari, J. P; Shelat, A. A.; Kosinski, A.; Caffrey, C. R.; Connelly, M.; Zhu, F.; McKerrow, J. H.; Guy, R. K. “Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB,” Bioorg. Med. Chem. Let., 2008, 18(9), 2883-85.

32. Arnold, A.; Ranaivo, P.; Guy, R. K. “Synthesis and Characterization of BODIPY-labeled Colchicine,” Bioorg. Med. Chem. Lett. 2008, 18(22), 5867-5870.

33. Feau, C.; Arnold, L. A.; Kosinski, A; Guy, R. K. “A high throughput Ligand Competition

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Binding Assay for the Androgen Receptor and other Nuclear Receptors,” J. Biomol. Screen. 2008, 14(1), 43-48.

34. Teichert, A.; Arnold, A.; Otieno, S.; Oda, Y.; Augustinaite, I.; Geistlinger, T. R.; Kriwacki, R. W.; Guy, R. K.; Bikle, D. D. “Differential Binding of Coregulator Motifs to the Vitamin D Receptor: Regulation by Ligand,” Biochemistry, 2009, 48(7), 1454-1461.

35. Jones, J. O.; Bolton, E. C.; Huang, Y.; Feau, C.; Guy, R. K.; Yamamoto, K. R.; Hann, B.; Diamond, M. I. “Ligand Independent Androgen Receptor Inhibition in vitro and in vivo,” Proc. Natl. Acad. Sci. USA, 2009, 106(17), 7233-8..

36. Shahian, T.; Lee, G. M.; Lazic, A.; Arnold, L. A.; Velusamy, P.; Roels, C. M.; Guy, R. K.; Craik, C. S. “Inhibition of a Viral Enzyme by a Small Molecule Dimer Disrupter,” Nature Chem. Biol., 2009, 5(9), 640-646.

37. Mallari, J; Guigemde, W. A.; Guy, R. K. “Antimalarial activity of thiosemicarbazones and purine derived nitriles,” Bioorg. Med. Chem. Lett. 2009, 19(13), 3546-3549.

38. Hwang, J. Y.; Arnold, L. A.; Zhu, F.; Kosinski, A.; Mangano, T. J.; Setola, V.; Roth, B. L.; Guy, R. K. “Improvement of Pharmacological Properties of Irreversible Thyroid Receptor Coactivator Binding Inhibitors,” J. Med. Chem., 2009, 52(13), 3892-3901.

39. Feau, C.; Arnold, L. A.; Kosinski, A.; Zhu, F.; Connelly, M.; Guy, R. K. “Novel Flufenamic Acid Analogs as Inhibitors of Androgen Receptor Mediated Transcription,” ACS Chem. Biol., 2009, 4(10), 834-843.

40. Margolis, R. N.; Moore, D. D.; Wilson, T. M.; Guy, R. K. “Chemical Approaches to Nuclear Receptors in Metabolism,” Sci. Signal 2009, 2(82), mr5.

41. Mallari, J.; Shelat, A.; Kosinski, A.; Caffrey, C.; Connelly, M.; Zhu, F.; McKerrow, J.; Guy, R. K. “Structure-guided Development of Selective TbCatB Inhibitors,” J. Med. Chem., 2009, 52(20), 6489-6493.

42. Smithson, D. C.; Shelat, A. A.; Baldwin, J.; Phillips, M. A.; Guy, R. K. “Optimization of a Non-Radioactive High-Throughput Assay for Decarboxylase Enzymes,” Assay Drug Dev. Technol., 2010, 8(2), 175-175.

43. Hwang, J. Y.; Smithson, D. C.; Connelly, M.; Maier, J.; Zhu, F.; Guy, R. K. “Discovery of halo-nitrobenzamides with potential application for Human African Trypanosomiasis,” Bioorg. Med. Chem. Lett. 2010, 20(1), 149-152.

44. Smithson, D. C.; Lee, J.; Shelat, A. A.; Phillips, M. A.; Guy, R. K. “Discovery of Potent and Selective Inhibitors of Trypanosoma brucei Ornithine Decarboxylase,” J. Biol. Chem. 2010, 285(22), 16771-16781.

45. Uddin, M. J.; Smithson, D. C.; Brown, K.’ Crews, B. C.; Connelly, M.; Marnett, L. J.; Guy, R. K. “Podophyllotoxin Analogues Active Against Trypanosoma brucei,” Bioorg. Med. Chem. Lett., 2010, 20(5), 1787-1791. PMCID: PMC2826502

46. Reed, D.; Ying, S.; Shelat, A.; Mills, N.; Smithson, D.; Arnold, A.; Otieno, S.; Regni, C.; Zhu, F.; Kriwacki, R.; Schulman, B.; Guy, R. K.; Dyer, M. A. “Identification and Characterization of a Small Molecule Inhibitor of MDMX,” J. Biol. Chem. 2010, 286(14), 10786-10796. PMCID: PMC2856285

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47. Zhang, Y.; Guiguemde, W. A.; Sigal, M.; Zhu, F.; Connelly, M. C.; Nwaka, S.; Guy, R. K. “Synthesis and Structure-Activity Relationships of Antimalarial 4-oxo-3-carboxyl Quinolones,” Bioorg. Med. Chem. 2010, 18(7), 2756-2766. PMCID: PMC2850272.

48. Tu, Y.; Jeffries, C.; Ruan, H.; Nelson, C.; Smithson, D.; Shelat, A. A.’ Li, X.C.; Hester, J. P.; Smillie, T.; Khan, I. A.; Walker, L.; Guy, R. K.; Yan, B. “An Automated High-Throughput System to Fractionate Natural Products for Drug Discovery,” J. Nat. Prod., 2010, 73(4), 751-754. PMCID: PMC2866159

49. Ray, S.; Madrid, P.; Catz, P.; LeValley, S.; Furniss, M.; Guy, R. K.; Derisi, J.; Iyer, L.; Green, C.; Mirsalis, J. “Development of a New Generation of 4-Aminoquinoline Antimalarials Using Predictive Pharmacokinetic and Toxicology Models,” J. Med. Chem. 2010, 53(9), 3685-3695. PMCID: PMC2866084

50. Guiguemde, W. A.; Shelat, A. A.; Bouck, D.; Duffy, S.; Crowther, G. J.; Davis, P. H.; Smithson, D.; Connelly, M.; Clark, J.; Zhu, F.; Jimenez-Diaz, M. B.; Martinez, M. S.; Wilson, E.; Tripathy, A. K.; Gut, J.; Sharlow, E. R.; Bathurst, I.; Mazouni, F. E.; Fowble, J. W.; Forquer, I.; Angulo-Barturen, I.; Ferrer, S.; Rosenthal, P. J.; DeRisi, J. L.; Sullivan, D. J.; Lazo, J. S.; Roos, D. S.; Riscoe, M. K.; Phillips, M. A.; Rathod, P. K.; Van Voorhis, W. C.; Avery, V. M.; Guy, R. K. “Chemical Genetics of Plasmodium Falciparum,” Nature, 2010, 465(7296), 311-315. PMCID: PMC2874979

51. Mallari, J. P.; Zhu, F.; Lemoff, A.; Kaiser, M.; Lu, M.; Brun, R.; Guy, R. K., “Optimization of Purine-Nitrile TbcatB Inhibitors for use In Vivo and Evaluation of Efficacy in Murine Models,” Bioorg. Med. Chem. 2010, 18(23), 8302-8309. PMCID: PMC21051236.

52. Zhang, Y.; Anderson, M.; Weisman, J. L.; Lu, M.; Choy, C. J.; Boyd, V. A.; Price, J.; Sigal, M.; Clark, J.; Connelly, M.; Zhu, F.; Guiguemde, W. A.; Jeffries, C.; Yang, L.; Lemoff, A.; Liou, A. P.; Webb, T. R.; DeRisi, J. L.; Guy, R. K. “Evaluation of Diarylureas for Activity against Plasmodium Falciparum,” ACS Med Chem Lett, 2010, 1(9), 460-465. PMCID: PMC3019604.

53. Feau, C.; Arnold, L. A.; Kosinski, A.; Guy, R. K. “Ligand Competition Binding Assay for the Androgen Receptor,” Meth. Mol. Biol., 2011, 776, 59-68. PMCID: PMC2632761.

54. De Leon, J. T.; Iwai, A.; Feau, C.; Garcia, Y.; Balsiger, H. A.; Storer, C.; Lee, S.; Kim, Y. S.; Chen, Y.; Ning, Y.-M.; Riggs, D. L.; Trepel, J.; Guy, R. K.; Fletterick, R.; Neckers, L. M.; Cox, M. B. “A Distinct Class of Nuclear Receptor Alternate Site Modulators (NRAMS) that Target the Regulation of Androgen Receptor by the Cochaperone FKBP52,” Proc. Natl Acad. Sci. USA. 2011, 108(29), 11878-11883. PMCID: PMC3141981.

55. Zhang, F.; Tagen, M.; Throm, S.; Mallari, J.; Miller, L.; Guy, R. K.; Dyer, M. A.; Williams, R. T.; Roussel, M. F.; Nemeth, K.; Zhu, F.; Zhang, J.; Lu, M.; Stewart, C. F.; “Whole Body Physiologically Based Pharmacokinetic Model for Nutlin-3a in Mice after Intravenous and Oral Administration,” Drug Disp. Met. 2011, 39(1), 15-21. PMCID: 20947617.

56. Brennan, R. C.; Federico, S.; Bradley, C.; Zhang, J. Flores-Otero, J.; Wilson, M.; Stewart, C.; Zhu, F.; Guy, K., Dyer, M. A. “Targeting the p53 Pathway in Retinoblastoma with Subconjunctival Nutlin-3a,” Cancer Research, 2011, 71(12), 4205-4213. PMCID: PMC3116943.

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57. Lack, N. A.; Axerio, P.; Tavassoli, P.; Kuchenbecker, K.; Han, F. Q.; Chan, K. H.; Feau, C.; LeBlanc, E.; Guns, E.; Guy, R. K.; Rennie, P. S.; Cherkasov, A., “Targeting the BF3 pocket of the Androgen Receptor through in silico molecular modeling,” J. Med. Chem. 2011, 54(24), 8563-8573, PMCID: PMC3668559.

58. Hwang, J. Y.; Huang, W.; Arnold, L. A.; Huang, R.; Attia, R. R., Connelly, M.; Wichterman, J.; Zhu, F, Augustinaite, I.; Austin, C.P.; Inglese, J.; Johnson, R. L.; Guy, R. K.; “Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone,” J. Biol. Chem. 2011, 286(14),11895-908. PMCID: PMC3069392.

59. Zhang, F.; Throm, S. L.; Murley, L. L.; Miller, L. A.; Zatechka, D. S.; Guy, R. K.; Kennedy, R.; Stewart, C. F.; “MDM2 Antagonist Nutlin-3a Reverses Mitoxantrone Resistance by Inhibiting Breast Cancer Resistance Protein Mediated Drug Transport,” Biochem. Pharmacol. 2011, 82(1), 24-34. PMCID: PMC3108438

60. Johnson, R. L.; Hwang, J. Y.; Arnold, L. A.; Huang, R.; Wichterman, J.; Augustinaite, I.; Austin, C. P.; Inglese, J.; Guy, R. K.; Huang, W. “A Quantitative High Throughput Screen Identifies Novel Inhibitors of the Interaction of Thyroid Receptor β with a Peptide Ligand of Steroid Receptor Coactivator 2,” J. Biomolecular Screen. 2011, 16(6), 618-627. PMCID: PMC3162318.

61. Cui, J.; Chai, S. C.; Shelat, A.; Guy, R. Kiplin, Chen, T. “An Automated Approach to Efficiently Reformat a Large Collection of Compounds,” Current Chemical Genetics, 2011, 5, 42-7. PMCID: PMC3145259.

62. Atkinson, J.; Shelat, A. A.; Carcaboso, A. M.; Kranenburg, T. A.; Arnold, A.; Wright, K.; Johnson, R. A.; Poppleton, H.; Mohankumar, K. M.; Feau, C.; Phoenix, T.; Gibson, P.; Zhu, L.; Tong, Y.; Eden, C.; Priebe, W.; Koul, D.; Yung, W. K. A.; Gajjar, A.; Stewart, C. F.; Guy, R. K.; Gilbertson, R. J. “Integrated In Vitro and In Vivo Screening of Tumor and Normal Neural Stem Cells Identifies Potential New Treatments of Ependymoma,” Cancer Cell, 2011, 20(3), 384-399. PMCID: PMC3172881.

63. Sadana, P.; Hwang, J.-Y.; Attia, R.; Arnold, A.; Neale, G.; Guy, R. K. “Similarities and Differences between Two Modes of Antagonism of the Thyroid Hormone Receptor,” ACS Chemical Biology, 2011, 6(10), 1096-1106. PMCID: PMC3199310.

64. Lowes, D.; Guiguemde, W. A.; Connelly, M.; Zhu, F.; Sigal, M.; Clark, J.; Lemoff, A.; DeRisi, J.; Wilson, E.; Guy, R. Kiplin, “The Optimization of Propafenone Analogues as Anti-Malarial Leads,” J. Med. Chem., 2011, 54(20), 7477-7485. PMCID: PMC3208124.

65. Hwang, J.-Y.; Kawasuji, T.; Lowes, D.; Clark, J.; Connelly, M.; Zhu, F.; Guiguemde, W. A.; Sigal, M.; Wilson, E.; DeRisi, J. L.; Guy, R. K., “Synthesis and Evaluation of 7-Substituted 4-Aminoquinoline Analogs for Antimalarial Activity,” J. Med. Chem. 2011, 54(20), 7084-7093.PMCID: PMC3594046.

66. Guo, J.; Guiguemde, W. A.; Bentura-Marciano, A.; Clark, J.; Haynes, K. R.; Wing-Chi, C.; Ho-Ning, W.; Hunt, N.; Guy, R. K.; Golenser, J. “Synthesis of Artemiside and its Effects in Combination with Conventional Drugs Against Severe Malaria,” Antimicrob. Agent. Chemother. 2012, 56(1), 163-173. PMCID: PMC3256061.

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67. Guiguemde, W. A.; Shelat, A. A.; Garcia-Bustos, J. F.; Diagana, T. T.; Gamo, F. J.; Guy, R. K. “Global Phenotypic Screening for Antimalarials,” Chem. Biol., 2012, 19(1), 116-129.

68. Hwang, J.; Attia, R.; Zhu, F.; Lemoff, A.; Jeffries, C.; Connelly, M.; Guy, R. K. “Synthesis and Evaluation of Sulfonylnitrophenylthiazoles (SNPT’s) as Thyroid Hormone Receptor-Coactivator Interaction Inhibitors,” J. Med. Chem. 2012, 55(5), 2301-2310. PMCID: PMC3308170.

69. Zhang, Y.; Clark, J. A.; Connelly, M. C.; Zhu, F.; Guiguemde, W. A.; Pradhan, A.; Iyer, L.; Furimsky, A.; Gow, J.; Parman, T.; El Mazouni, F.; Phillips, M. A.; Kyle, D. E.; Mirsalis, J.; Guy, R. K.; “Lead Optimization of 3-Carboxyl-4(1H)-Quinolones to Deliver Orally Bioavailable Antimalarials,” J. Med. Chem., 2012, 55(9), 4205-4219. PMCID: PMC3349818

70. Nandikonda, P.; Lynt, W. Z.; McCallum, M. M.; Ara, T.; Baranowski, A. M.; Yuan, N. Y.; Pearson, D.; Bikle, D. D.; Guy, R. K.; Arnold, L. A. “Discovery of the First Irreversible Small Molecule Inhibitors of the Interaction Between the Vitamin D Receptor and Coactivators,” J. Med. Chem. 2012, 55(10) 4640-4651. PMCID: PMC3364162.

71. Guiguemde, W. A.; Guy, R. K. “An All Purpose Antimalarial Drug Target,” Cell Host & Microbe, 2012, 11(6), 555-557.

72. Lowes, D.; Pradhan, A.; Iyer, L.; Parfan, T.; Gow, J.; Zhu, F.; Furimsky; Lemoff, A.; Guiguemde, W. A.; Sigal, M.; Clark, J.; Wilson, E.; Tang, L.; Connelly, M. DeRisi, J.; Kyle, D. E.; Mirsalis, J.; Guy, R. K.; “Lead Optimization of Antimalarial Propafenone Analogs,” J. Med. Chem., 2012, 55(12), 6087-6093. PMCID:PMC4408918.

73. Zhang, L.; Fourches, D.; Sedykh, A.; Zhu, H.; Golbraikh, A.; Ekins, S.; Clark, J.; Connelly, M. C.; Sigal, M.; Hodges, D.; Guiguemde, A.; Guy, R. K.; Tropsha, A.; “Discovery of Novel Antimalarial Compounds Enabled by QSAR-based Virtual Screening,” J. Chem. Info. Model., 2013, 53(2), 475-492. PMCID:PMC3644566.

74. Cloete, T. T.; Krebs, H. J.; Clark, J. A.; Connelly, M. C.; Orcutt, A.; Sigal, M. S.; Guy, R. K.; N’Da, D. D. “Synthesis and Antimalarial Activity of 10-Alkyl/aryl Esters and Aminoethylethers of Artemisinin,” Bioorg. Chem. 2012, 46C, 10-16. PMCID: Not applicable.

75. Hwang, J.-Y.; Attia, R. R.; Carrillo, A. Connelly, M. C.; Guy, R. K.; “Synthesis and evaluation of methylsulfonylnitrobenzamides (MSNBA) as inhibitors of the thyroid hormone receptor-coactivator interaction,” Bioorg. Med. Chem. Lett. 2013, 23(6), 1891-1895. PMCID: PMC3594046

76. N’Da, D.; Lombard, M.; Clark, J.’ Connelly, M.; Matheny, A.; Sigal, M.; Guy, R. “Antiplasmodial activity and cytotoxicity of 10β-aminoquinolinylethylethers of artemisinin,” Drug Res. 2013, 63(2), 104-108. PMCID: Not applicable.

77. Nilsen, A.; LaCrue, A.; White, K. L.; Forquer, I. P.; Cross, R. M.; Marfurt, J.; Mather, M. W.; Delves, M. J.; Shackleford , D. M.; Saenz, F. E.; Morrisey, J. M.; Steuten, J.; Mutka, T.; Li, Y.; Wirjanata, G.; Ryan, E.; Duffy, S.; Kelly, J. X.; Sebayang, B. F.; Zeeman, A.-M.; Noviyanti, R.; Sinden, R. E.; Kocken, C. H. M.; Price, R. N.; Avery, V. M.; Angulo-Barturen, I.; Jimenez-Diaz, M. B.; Ferrer, S.; Herreros, E.; Sanz, L. M.; Gamo, F. J.; Bathurst, I.; Burrows, J.; Siegl, P.; Guy, R. K.; Winter, R. W.; Vaidya, A. B.; Charman, S. A.; Kyle, D. E.; Manetsch, R.; Riscoe, M. K. “Quinolone-3-Diarylethers: A new class of

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drugs for a new era of malaria eradication,” Sci. Trans. Med. 2013, 5(177):177ra37. PMCID: PMC4227885.

78. Hwang, J.-Y.; Smithson, D.; Zhu, F.; Holbrook, G.; Connelly, M.; Kaiser, M.; Brun, R.; Guy, R. K. “Optimization of Chloronitrobenzamides (CNBs) as Therapeutic Leads for Human African Trypanosomiasis (HAT),” J. Med. Chem.2013, 56(7), 2850-2860. PMCID: Not applicable.

79. Vrijens, K.; Lin, W.; Cui, J.; Farmer, D.; Low, J.; Pronier, E.; Feng, F. Y.; Shelat, A. A.; Guy, R. K.; Taylor, M. R.; Chen, T; Roussel, M. F. “Identification of small molecule activators of BMP signaling,” PLoS One, 2013, 8(3):e59045. PMCID: PMC3602516

80. Hooft van Huijsduijnen, R. H.; Guy, R. K.; Chibale, K.; Haynes, R. K.; Peitz, I.; Kelter, G.; Phillips, M. A.; Vennerstrom, J. L.; Yuthavong, Y. Wells, T. N. C. “Anticancer Properties of Distinct Antimalarial Drug Classes,” PLOS One, 2013, 8(12):e82962. PMCID: PMC3877007

81. Derbyshire, E. R.; Min, J.; Guiguemde, W. A.; Clark, J. A.; Connelly, M. C.; Magalhaes, A. D.; Guy, R. K.; Clardy, J. “Dihydroquinazolinone Inhibitors of Proliferation of Blood and Liver Stage Malaria Parasites,” Antimicrob. Agents Chemother.2013, 8(12), 1516-1522. PMCID: PMC3957893

82. Singh, H.; Shelat, A. A.; Singh, A.; Boulos, N.; Williams, R. T.; Guy, R. K. “A Screening-Based Approach to Circumvent Tumor Microenvironment-Driven Intrinsic Resistance to BCR-ABL+ Inhibitors in Ph+ Acute Lymphoblastic Leukemia.,” J. Biomol. Screen. 2014, 19(1), 158-167. PMCID:PMC3963394.

83. Guo, K.; Shelat, A.; Guy, R. K.; Kastan, M. B. “Development of a Cell-Based, High-Throughput Screen for ATM Kinase Inhibitors,” J. Biomol. Screening, 2014, 19(4), 538-546. PMCID: Not applicable

84. Yang, J.; Liang, Q.; Wang, M.; Jeffries, C.; Smithson, D.; Tu, Y.; Boulos, N.; Jacobs, M. R.; Shelat, A. A.; Wu, Y.; Ravu, R. R.; Gilbertson, R.; Avery, M. A.; Khan, I. A.; Walker, L. A.; Guy, R. K.; Li, X-C. “UPLC-MS-ELSD-PDA as A Powerful Dereplication Tool to Facilitate Compound Identification from Small Molecule Natural Product Libraries,” J. Nat. Prod., 2014, 77(4), 902-909. PMCID: Not applicable.

85. Morfouace, M.; Shelat, A.; Jacus, M.; Freeman, B. B.; Turner, D.; Robinson, S.; Zindy, F.; Wang, M.; Finkelstein, D.; Bihannic, L.; Puget, S.; Aryarult, O.; Robinson, G. W.; Li, X.-N.; Guy, R. K.; Stewart, C.; Gajjar, A.; Roussel, M. F. “Pemetrexed and Gemcitabine as Combination Therapy for the Treatment of Group3 Medulloblastoma,” Cancer Cell, 2014, 25(4), 516-529. PMCID: PMC3994669.

86. Lotharius, J.; Gamo-Benito, F. J.; Angulo-Barturen, I.; Clark, J.; Connelly, M.; Ferrer-Bazaga, S.; Parkinson, T.; Viswanath, P.; Bandodkar, B.; Rautela, N.; Bharath, S.; Duffy, S.; Avery, V.; Mohrle, J. J.; Guy, R. K.; Wells, T. “Repositioning: The Fast Track to New Anti-malarial Medicines,” Malaria J., 2014, 13, 143. PMCID: PMC3877007

87. Pritchard, E. M.; Stewart, E.; Zhu, F.; Bradley, C.; Griffiths, L.; Yang, L.; Suryadevara, P. K.; Zhang, J.; Freeman, B. B.; Guy. R. K.; Dyer, M. A. “Pharmacokinetics and Efficacy of the Spleen Tyrosine Kinase Inhibitor R406 after Ocular Delivery for Retinoblastoma,” Pharm. Res., 2014, 31(11), 3060-3072. PMCID: PMC4213378

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88. Wang, C.; Zhao, Q.; Min, J.; Muniyan, S.; Vargas, M.; Wang, X.; Dong, Y.; Guy, R. K.; Lin, M.-F.; Keiser, J.; Vennerstrom, J.; “Antischistosomal versus Antiandrogenic Properties of Aryl Hydrantoin Ro 12-3978,” Am. J. Trop. Med., 2014, 90(6), 1156-1158. PMCID: PMC4047746.

89. Guiguemde, A.; Hunt, N.; Guo, J.; Marciano, A.; Haynes, R.; Clark, J.; Guy, R. K.; Golenser, J. “Treatment of Murine Cerebral Malaria by Artemisone in Combination with Conventional Anti-malarial Drugs: Anti-Plasmodial Effects and Immune Responses,” Antimicrob. Agents Chemother, 2014, 58(8), 4745-4754. PMCID: PMC4135990.

90. Vara, B. A.; Mayasundari, A.; Tellis, J. C.; Danneman, M. W.; Arrendondo, V.; Davis, T. A.; Min, J.; Finch, K.; Guy, R. K.; Johnston, J. N. “Organocatalytic, Diastereo-and Enantioselective Synthesis of Nonsymmetric cis-Stilbene Diamines: A Platform for the Preparation of Single-Enantiomer cis-Imidazolines for Protein-Protein Inhibition,” J. Org. Chem. 2014, 79(15), 6913-6938. PMCID: PMC4120989

91. Jiménez-Díaz, M. B.; Ebert, D.; Salinas, Y.; Pradhan, A.; Lehane, A.; Myrand-Lapierref, M.-E.; O’Loughlin, K. G.; Shackleford, D. M.; Lage de Almeida, M. J.; Clark, J. A.; Dennis, A.; Diep, J.; Deng, X.; Endsley, A. N.; Fedewa, G.; Guiguemde, A.; Gomez-Lorenzo, M. G.; Holbrook, G.; Horst, J.; Kim, C.; Liu, J.; Lee, M. C. S.; Matheny, A.; Martínez, M. S.; Rodriguez-Alejandre, A.; Sanz, L.; Sigal, M. S.; Spillman, N.; Stein, P. D.; Wang, Z.; Zhu, F.; Waterson, D.; Knapp, S.; Fidock, D.; Gamo, F. J.; Charman, S. A.; Mirsalis, J. C.; Ma, H.; Ferrer, S.; Kirk, K.; Angulo-Barturen, I.; Kyle, D.; DeRisi, J. L.; Floyd, D. M.; Guy, R. K. “(+)-SJ733: A Clinical Candidate for Malaria that Acts Through ATP4 to Induce Rapid Host-Mediated Clearance of Plasmodium,” Proc. Natl. Acad. Sci. USA, 2014, 11(50), E5455-62. PMCID: PMC4273362.

92. Ortiz, D.; Guiguemde, W. A.; Johnson, A.; Elya, C.; Anderson, J.; Clark, J.; Connelly, M.; Yang, L.; Min, J.; Sato, Y.; Guy, R. K.; Landfrear, S. M. “Identification of Selective Inhibitors of the Plasmodium falciparum Hexose Transporter PfHT by Screening Focused Libraries of Anti-Malarial Compounds,” PLoS One, 2015, 10(4), e0123598. PMCID: PMC4404333.

93. Tanaka, T. Q.; Guiguemde, W. A.; Barnett, D. S.; Marion, M. I.; Min, J.; Connelly, M. C.; Suryadevara, P. K.; Guy, R. K.; Williamson, K. C. “Potent Plasmodium falciparum gametocytocidal activity of lead anti-malaria chemotype, diaminonaphthoquinones, identified in an anti-malaria compound screen,” Antimicrob. Agents Chemother. 2015, 59(3), 1389-1397. PMCID: PMC4325765.

94. Paugh, S. W.; Bonten, E. J.; Savic, D.; Ramsey, L. B.; Thierfelder, W. E.; Gurung, P.; Malireddi, R. K. S.; Actis, M.; Mayasundari, A.; Min, J.; Coss, D. R.; Laudermild, L. T.; Panetta, J. C.; McCorkle, J. R.; Fan, Y.; Crews, K. R.; Stocco, G.; Wilkinson, M. R.; Ferreira, A. M.; Cheng, C.; Yang, W.; Karol, S. E.; Fernandez, C. A. Diouf, B.; Smith, C.; Hicks, J. K.; Zanut, A.; Giordanengo, A.; Crona, D.; Bianchi, J. J.; Holmfeldt, L.; Mullighan, C. G.; den Boer, M. L.; Pieters, R.; Jeha, S.; Dunwell, T. L.; Latif, F.; Bhojwani, D.; Carroll, W. L.; Pui, C.-H.; Myers, R. M.; Guy, R. K.; Kanneganti, T.-D.; Relling, M. V.; Evans, W. E. “NALP3 inflammasome upregulation and CASP1 Cleavage of the Glucocorticoid Receptor Cause Glucocorticoid Resistance in Leukemia Cells,” Nat. Genetics, 2015, 47(6), 607-614. PMCID: PMC4449308

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95. Pettersson, M.; Bilman, D.; Jacobsson, J.; Nilsson, J. R.; Min, J.; Iconaru, L.; Guy, R. K.; Kriwacki, R. W.; Andreasson, J.; Grotli, M. “8-Triazolylpurines: Towards Fluorescent Inhibitors of the MDM2/p53 interaction,” PloS One, 2015, 10(5), e0124423. PMCID: PMC4420247.

96. Pettersson, M.; Quant, M.; Min, J.; Iconaru, L.; Kriwacki, R. W.; Waddell, M. B.; Guy, R. K.; Luthman, K.; Grotli, M., “Design, Synthesis and Evaluation of 2,5-Diketo-piperazines as Inhibitors of the MDM2-p53 Interaction,” PloS One, 2015, Oct 1;10(10):e0137867. PMCID: PMC4591261.

97. Ravu, R. R.; Jacob, M. R.; Jeffries, C.; Tu, Y.; Khan, S. I.; Agarwal, A. K.; Guy, R. K.; Walker, L. A.; Clark, A. M.; Li, X.-C. “Using LC-MS and 1H NMR as an Improved Dereplication Tool to Identify Antifungal Diterpenoids from Sagittaria latifolia,” Phytochem. 2015, 78(9), 2255-2259. PMCID: In progress.

98. Churchman, M. L.; Low, J.; Qu, C.; Paietta, E. M.; Kasper, L. H.; Chang, Y.; Payne-Turner, D.; Althoff, M. J.; Song, G.; Chen, S.-C.; Ma, J.; Rusch, M.; McGoldrick, D.; Edmonson, M.; Gupta, P.; Wang, Y.-D.; Caufield, W.; Freeman, B.; Li, L.; Panetta, J. C.; Baker, S.; Yang, Y.-L.; Roberts, K.; McCastlain, K.; Iacobucci, I.; Peters, J. L.; Centonze, V. E.; Notta, F.; Dobson, S. M.; Zandi, S.; Dick, J. E.; Janke, L. ;Peng, J.; Dodali, K.; Pagala, V.; Min, J.; Mayuasundari, A.; Williams, R. T.; Willman, C. L.; Rowe, J. M.; Luger, S.; Dickens, R. A.; Guy, R. K.; Chen, T.; Mulligan, C. G. “Efficacy of retinoids in IKZF1-mutated BCR-ABL1 acute lymphoblastic leukemia,” Cancer Cell, 2015, 28(3), 343-56. PMCID: PMC4573904.

99. Barnett, D. S.; Guy, R. K. “Antimalarials in Development in 2014,” Chem. Rev. 2014, in press. PMCID: PMC Journal – In progress

100. Carrillo, A.; Guy, R. K. “Evaluation of Histone Deacetylase Inhibitors (HDACi) as Therapeutic Leads for Human African Trypanosomiasis (HAT),” Bioorg. Med. Chem. 2015, 23(16), 5151-5. PMCID: Not Applicable

101. Verlinden, B.K.; de Beer, M.; Pachaiyappan, B.; Besaans, E.; Andayi, W. A.; Reader, J.; Niemand, J.; van Biljon, R.; Guy, R. K.; Egan, T.; Woster, P. M.; Birkholtz, L.-M. “Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites,” Bioorg. Med. Chem. 2015, in press

102. Pritchard, E. M.; Dyer, M. A.; Guy, R. K. “Progress in Small Molecule Therapeutics for the Treatment of Retinoblastoma,” Mini-Rev. Med. Chem. 2015, in press.

103. Bruhn, D. F.; Wyllie, S.; Rodriguez-Cortes, A.; Carrillo, A.; Rakesh, Rivas, F.; Guy, R. K.; Fairlamb, A. H.; Lee, R. E. “Pentacyclic Antitubercular Nitrofurans that Rapidly Kill Nifurtimox Resistant Trypanosomes,” J. Antimicrob. Ther. 2015, in press

104. Brennan, R. C.; Pritchard, E. M.; Guy, R. K.; Dyer, M. A.; Wilson, M. W. “Current and Emerging Therapy for Improving Outcomes in Patients with Intraocular Retinoblastoma,” Expert Opinion in Oncology, 2015, in revision

105. Min, J.; Guo, K.; Suryadevara, P. K.; Feau, C.; Young, B. M.; Holbrook, G.; Zhu, F.; Lemoff, A.; Connelly, M. C.; Kastan, M. B.; Guy, R. K. “Optimization of a Novel Series of ATM Inhibitors as Potential Radiosensitizing Agents,” J. Med. Chem. 2015, in revision.

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106. Barnett, D. S.; Min, J.; Jimenez-Diaz, M. B.; Lu, M.; Clark, J. A.; Martinez, M. S.; Delves, M.; Ruecker, A.; Pradhan, A.; Gow, J.; Connelly, M. C.; Holbrook, G.; Yang, L.; Zhu, F.; Viera, S.; Huertas, L.; Garuti, H.; Magan, N.; Cortes, L.; Gomez, V.; Straschil, U.; Parman, T.; Matheny, A.; Guiguemde, W. A.; Sigal, M. S.; Winzeler, E. A.; Mirsalis, J.; Kyle, D.; Sinden, R. E.; Ferrer, S.; Angulo-Barturen, I.; Waterson, D.; Guy, R. K. “Early Lead Optimization of Diaminonapthoquinones (DANQs) as Potential Antimalarial Agents,” J. Med. Chem. 2015, submitted.

107. Ban, D.; Royappa, G.; Park, C.-G.; Min, J.; Mayasundari, A.; Guy, R. K.; Kriwacki, R. “Identifying Unique Pertubations in Conformational Landscapes of Protein Drug Targets,” J. Am. Chem. Soc., 2015, submitted.

108. Min, J.; Arnold, L. A.; Attia, R. R.; Connelly, M.; Shelat, A.; Guy, R. K. “Inhibitors of the Interaction of PPARγ and SMRT,” J. Biol. Chem. 2014, submitted

Articles and Chapters in Books Chapters from Nicolaou Laboratory (Graduate School) 1. Nicolaou, K. C.; Guy, R. K. "Total Synthesis of Taxol and Designed Taxoids," New

Perspectives in Drug Design, 1995, 69-87. 2. Nicolaou, K. C.; Guy, R. K. "Total Synthesis of Taxol," Taxane Anticancer Agents: Basic

Science and Current Status, ACS Symposium Series 583, 302-312. 3. Nicolaou, K. C.; Guy, R. K. “Synthesis of Biologically Active Taxoids,” Chemistry and

Molecular Aspects of Drug Design and Action, 2008, 101-108. Chapters from Guy Laboratory (UCSF) 1. Geistlinger, T. R.; Guy, R. K. “Selective inhibitors of nuclear hormone receptor coactivator

binding,” Methods Enzymol. 2003, 364, 223-46. 2. Fujii, N.; Haresco, J. J.; Pendola-Novak, K. A.; Stokoe, D.; Gage, M.; Von Zastrow, M.;

Kuntz, I. D.; Guy, R. K. “Design and Synthesis of Inhibitors of the PDZ Protein Interaction Domain,” Innov. Persp. Solid Phase Synth. & Combi. Chem. Lib. 2004, 8, 163-166.

3. Moore, J. M.; Guy, R. K.; “Co-regulators of Thyroid Hormone Receptor Signaling,” Clinical Proteomics, 2004, 4, 475-482.

Chapters from Guy Laboratory (SJCRH) 1. Smithson, D.; Guiguemde, A.; Guy, R. K. “Antimalarials,” in in Burger’s Medicinal

Chemistry Volume 7, 7th Edition, eds. Abraham, D. J.; Rotella, D. P. (Hoboken: Wiley 2010), 603-712.

Patents Patents from Nicolaou Laboratory (Graduate School) 1. Nicolaou, K. C.; Nantermet, P. G.; Guy, R. K.; Ueno, H. “Transformations of Taxols,” US

Patent No. 6,043,382 2. Nicolaou, K. C.; Nantermet, P. G.; Guy, R. K.; Ueno, H. “Transformations of Taxols,” US

Patent No. 5,786,489 3. Nicolaou, K. C.; Nantermet, P. G.; Guy, R. K.; Ueno, H. “Transformations of Taxols,” US

Patent No. 5,504,222

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4. Nicolaou, K. C.; Nantermet, P. G.; Guy, R. K.; Ueno, H. “Access to Taxol Analogs,” US Patent No. 5,750,691

5. Nicolaou, K. C.; Nantermet, P. G.; Guy, R. K.; Ueno, H. “Access to Taxol Analogs,” US Patent No. 5,440,057

6. Nicolaou, K. C.; Wrasidlo, W.; Guy, R. K.; Pitsinos, E. “Water Soluble Onium Salt of Taxo-Diterpenoid,” US Patent No 6,025,491

7. Nicolaou, K. C.; Wrasidlo, W.; Guy, R. K.; Pitsinos, E. “Chemical Switching of Taxo-Diterpenoids between Low Solubility Active Forms and High Solubility Inactive Forms,” US Patent No. 6,252,094

8. Nicolaou, K. C.; Wrasidlo, W.; Guy, R. K.; Pitsinos, E. “Self-Assembled Taxo-Diterpenoid Nanostructures,” US Patent No. 6,271,384

Patents and Patent Applications from Guy Laboratory (UCSF) 1. Guy, R. K.; Kuntz, I. D.; Haresco, J.; Fujii, N. “Small Molecule Inhibition of a PDZ-domain

Interaction,” US Patent No. 7,141,600 2. Verkman, A.; Ma, T.; Guy, R. K. “Compounds Having Activity In Increasing Ion Transport

By Mutant-CFTR and Uses Thereof,” US Patent No. 7,939,558 3. Verkman, A.; Galietta, L. J. V.; Guy, R. K. “Compounds Having Activity in Increasing Ion

Transport by Mutant-CFTR and Uses Thereof,” US Patent No. 7,696,244 4. Guy; R. K.; Kuntz; I. D.; Haresco; J.; Fujii; N.; Novak; K. P.; Stokoe; D.; He; B.; You; L.;

Xu; Z.; Jablons; D. M. “Small Molecule Inhibition of PDZ-Domain Interaction,” US Patent No. 7,601,750

5. Guy; R. K.; Kuntz; I. D.; Haresco; J.; Fujii; N.; Novak; K. P.; Stokoe; D.; He; B.; You; L.; Xu; Z.; Jablons; D. M. “Small Molecule Inhibition of PDZ-Domain Interaction,” US Patent No. 7,141,600

6. Guy, R. K.; Fujii, N.; You, L.; Jablons, D. M. “Small Molecule Inhibition of PDZ-Domain Interaction,” US Patent No 7,795,295

7. Guy, R. K.; Fujii, N.; You, L.; Jablons, D. M. “Small Molecule Inhibition of PDZ-Domain Interaction,” US Patent No 8,211,934

8. Guy, R. K.; Kuntz, I. D.; Lu, F. “Alpha-helix Mimicry by a Class of Organic Molecules,” USPA 20030149038 US Patent Pending

9. Guy, R. K.; Moore, J. M. R.; Geistlinger, T. R. “Method for Obtaining the Binding Affinities of a Peptide Library to a Protein,” USPA 20040005636 US Patent Pending

10. James, T. L.; Lind, K. E; Du, Z.; Peterlin, B. M; Guy, R. K.; Madrid, P. B.; Mayer, M.; Fujinaga, K. “Inhibition of RNA Function,” USPA 20030229082 US Patent Pending

Patents and Patent Applications from Guy Laboratory (SJCRH) 1. Dyer, M. A.; Marine, J.C.; Jochemsen, A. G.; Guy, R. K. “Method for Treating Ocular

Cancer,” US Patent No. 8,470,785 2. Guy, R. K.; Zhu, F.; Clark, J.; Guiguemde, A.; Floyd, D.; Knapp, S.; Stein, P.; Castro, S.

“Substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides for Antimalarial Therapies,” USPA 20140235593

3. Guy, R.K.; Zhang, Y.; Young, B.; Dyer, M. A.; Finch, K.; Bashford, D.; Bharatham, N.; Kriwacki, R.; Royappa, G.; Min, L.; Min, J.; Ferreira, A. “Aryl-Substituted Imidazoles,” USPA 20130345237

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4. Singh, H.; Williams, R. T.; Guy, R. K. “Methods and Compositions for the Treatment of BCR-Abl Positive Lymphoblastic Leukemias,” Provisional Application