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TitleStructural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPAR gamma Drug Pioglitazone.
Journal, issue, pagesJ. Med. Chem., Vol. 62, Page 2008-2023, Year 2019
Publish dateMay 18, 2018 (structure data deposition date)
AuthorsMosure, S.A. / Shang, J. / Eberhardt, J. / Brust, R. / Zheng, J. / Griffin, P.R. / Forli, S. / Kojetin, D.J.
External linksJ. Med. Chem. / PubMed:30676741
MethodsX-ray diffraction
Resolution1.88 Å
Structure data

PDB-6dha:
Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Hydroxy Pioglitazone (M-IV)
Method: X-RAY DIFFRACTION / Resolution: 1.88 Å

Chemicals

ChemComp-GFV:
Hydroxy Pioglitazone (M-IV)

ChemComp-KNA:
nonanoic acid

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
Keywordstranscription/transcription inhibitor / Nuclear receptors / TZDs / Drug design / Therapeutic targets / TRANSCRIPTION / TRANSCRIPTION-TRANSCRIPTION INHIBITOR complex

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