nuclear receptor structures
Post on 31-Dec-2015
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Nuclear Receptor structures
Simon FolkertsmaSimon Folkertsma
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
Domain organization
DNA binding domain (DBD) Ligand binding domain (LBD)
Mechanism
3D Structure NR LBD
(hER)
Aligned structuresAligned structures
NR mechanism
apo agonist antagonist
Apo
NR mechanism
apo agonist antagonist
Agonist
NR mechanism
apo agonist antagonist
Antagonist
- 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?
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