Download - Druggable Genome and Proteome
DRUGGABLE GENOME AND PROTEOME
Karen A. Méndez L
“the most fruitful basis for the discovery of a new drug is to start with an old drug” (James W Black,
Nobel de Medicina 1988)
Druggability
Thomas H Keller, et al. Current Opinion in Chemical Biology 2006, 10:357–361
Drug- like compounds
Thomas H Keller, et al. Current Opinion in Chemical Biology 2006, 10:357–361
Lipinski (2001) --˃ Rule of 5 (RO5)
Rule of 5
1. RO5 applies only to compounds that are delivered by the oral route.
2. RO5 applies only to compounds that are absorbed by passive mechanisms
3. There are important exceptions (MW and natural compounds).
4. RO5 compliant compounds are not automatically good drugs
Disease and Druggable Genome
Dixon SJ and Stockwell BR (2009)
Hopkins y Groom (2002)
Overington et al. Nature Reviews Drug Discovery 5, 993–996 (December 2006) | doi:10.1038/nrd2199
Druggable Proteome
Door: ProteinLock: Drug Binding SiteKey: Drug
Pharmaceutically Tractable Genome
Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007
Druggable Network
Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007
Distribution of Drugs and Drug Targets
Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007
Distribution of Drugs and Drug Targets
Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007
References
Dixon SJ and Stockwell BR (2009) Identifying druggable disease-modifying gene products, Curr Opin Chem Biol 13: 549–555
Yıldırım et al, Drug–target network. NATURE BIOTECHNOLOGY VOLUME 25 NUMBER 10 OCTOBER 2007
Overington et al. Nature Reviews Drug Discovery 5, 993–996 (December 2006) | doi:10.1038/nrd2199
Thomas H Keller, et al. Current Opinion in Chemical Biology 2006, 10:357–361
Zheng CJ et al. (2006) Therapeutic Targets: Progress of Their Exploration and Investigation of Their Characteristics,
Pharmacol Rev 58: 259–279 Russ AP and Lampel S (2005) The druggable genome:an
update, Drug Discov Today 10 (23/24): 1607-1610 Hopkins AL and Groom CR (2002) The druggable genome,
Nat Rev Drug Discov 1: 727-730