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TitleDiscovery of a "Gatekeeper" Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers.
Journal, issue, pagesJ. Med. Chem., Vol. 64, Page 430-439, Year 2021
Publish dateJun 27, 2020 (structure data deposition date)
AuthorsWatanabe, M. / Fujihara, M. / Motoyama, T. / Kawasaki, M. / Yamada, S. / Takamura, Y. / Ito, S. / Makishima, M. / Nakano, S. / Kakuta, H.
External linksJ. Med. Chem. / PubMed:33356247
MethodsX-ray diffraction
Resolution2.15 Å
Structure data

PDB-7cfo:
Crystal structure of human RXRalpha ligand binding domain complexed with CBTF-EE.
Method: X-RAY DIFFRACTION / Resolution: 2.15 Å

Chemicals

ChemComp-WZ6:
1-[3-(2-ethoxyethoxy)-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl]-2-(trifluoromethyl)benzimidazole-5-carboxylic acid

ChemComp-GOL:
GLYCEROL

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsNUCLEAR PROTEIN / Retinoid X receptor alpha / antagonist

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