nuclear receptor structures
DESCRIPTION
Nuclear Receptor structures. Simon Folkertsma. Nuclear Receptors. ligand-inducible transcription factors ligands are lipophilic compounds 48 human NRs identified key processes are regulated by NRs (homeostasis, dif- ferentiation, embryonic development and organ physiology) - PowerPoint PPT PresentationTRANSCRIPT
![Page 1: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/1.jpg)
Nuclear Receptor structures
Simon FolkertsmaSimon Folkertsma
![Page 2: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/2.jpg)
Nuclear Receptors
ligand-inducible transcription factorsligands are lipophilic compounds48 human NRs identifiedkey processes are regulated by NRs (homeostasis, dif-ferentiation, embryonic development and organ physiology)diseases: cancer, diabetes, and osteoporosis
Important target for pharmaceutical industry
![Page 3: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/3.jpg)
Domain organization
DNA binding domain (DBD) Ligand binding domain (LBD)
![Page 4: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/4.jpg)
Mechanism
![Page 5: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/5.jpg)
3D Structure NR LBD
(hER)
![Page 6: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/6.jpg)
![Page 7: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/7.jpg)
Aligned structuresAligned structures
![Page 8: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/8.jpg)
NR mechanism
apo agonist antagonist
![Page 9: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/9.jpg)
Apo
![Page 10: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/10.jpg)
NR mechanism
apo agonist antagonist
![Page 11: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/11.jpg)
Agonist
![Page 12: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/12.jpg)
NR mechanism
apo agonist antagonist
![Page 13: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/13.jpg)
Antagonist
![Page 14: Nuclear Receptor structures](https://reader036.vdocuments.net/reader036/viewer/2022062314/56812eab550346895d944df9/html5/thumbnails/14.jpg)
- Where does the ligand bind?- Where is H12?- Where does the cofactor bind?- Is the compound an agonist or antagonist?- Can you find all twelve helices? - Are there hydrogen bonds between the ligand and the protein?