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TitlePPAR gamma Corepression Involves Alternate Ligand Conformation and Inflation of H12 Ensembles.
Journal, issue, pagesAcs Chem. Biol., Vol. 18, Page 1115-1123, Year 2023
Publish dateNov 5, 2021 (structure data deposition date)
AuthorsFrkic, R.L. / Pederick, J.L. / Horsfall, A.J. / Jovcevski, B. / Crame, E.E. / Kowalczyk, W. / Pukala, T.L. / Chang, M.R. / Zheng, J. / Blayo, A.L. ...Frkic, R.L. / Pederick, J.L. / Horsfall, A.J. / Jovcevski, B. / Crame, E.E. / Kowalczyk, W. / Pukala, T.L. / Chang, M.R. / Zheng, J. / Blayo, A.L. / Abell, A.D. / Kamenecka, T.M. / Harbort, J.S. / Harmer, J.R. / Griffin, P.R. / Bruning, J.B.
External linksAcs Chem. Biol. / PubMed:37146157
MethodsX-ray diffraction
Resolution2.499 - 2.6 Å
Structure data

PDB-7sqa:
PPAR gamma LBD bound to SR10221 and SMRT corepressor motif
Method: X-RAY DIFFRACTION / Resolution: 2.499 Å

PDB-7sqb:
PPAR gamma LBD bound to Inverse Agonist SR10221
Method: X-RAY DIFFRACTION / Resolution: 2.6 Å

Chemicals

ChemComp-A8R:
(2S)-2-{5-[(5-{[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]-2-chlorophenoxy}propanoic acid

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / Inverse agonist / Nuclear receptor / Ligand binding domain / corepressor / Helix 12

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