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3FC6

hRXRalpha & mLXRalpha with an indole Pharmacophore, SB786875

Summary for 3FC6
Entry DOI10.2210/pdb3fc6/pdb
DescriptorRetinoic acid receptor RXR-alpha, Nr1h3 protein, RETINOIC ACID, ... (5 entities in total)
Functional Keywordsliver x receptor, nuclear hormone receptors, agonists, epoxycholesterol, dna-binding, host-virus interaction, metal-binding, nucleus, polymorphism, receptor, transcription, transcription regulation, ubl conjugation, zinc, zinc-finger
Biological sourceHomo sapiens (human)
More
Cellular locationNucleus: P19793
Total number of polymer chains4
Total formula weight117308.05
Authors
Washburn, D.G.,Hoang, T.H.,Campobasso, N.,Smallwood, A.,Parks, D.J.,Webb, C.L.,Frank, K.,Nord, M.,Duraiswami, C.,Evans, C.,Jaye, M.,Thompson, S.K. (deposition date: 2008-11-21, release date: 2009-02-10, Last modification date: 2023-12-27)
Primary citationWashburn, D.G.,Hoang, T.H.,Campobasso, N.,Smallwood, A.,Parks, D.J.,Webb, C.L.,Frank, K.A.,Nord, M.,Duraiswami, C.,Evans, C.,Jaye, M.,Thompson, S.K.
Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.
Bioorg.Med.Chem.Lett., 19:1097-1100, 2009
Cited by
PubMed Abstract: A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRalpha will be disclosed.
PubMed: 19167885
DOI: 10.1016/j.bmcl.2009.01.004
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.063 Å)
Structure validation

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