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Structure paper

TitleIdentification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 19, Page 3550-3554, Year 2009
Publish dateApr 6, 2009 (structure data deposition date)
AuthorsConnors, R.V. / Wang, Z. / Harrison, M. / Zhang, A. / Wanska, M. / Hiscock, S. / Fox, B. / Dore, M. / Labelle, M. / Sudom, A. ...Connors, R.V. / Wang, Z. / Harrison, M. / Zhang, A. / Wanska, M. / Hiscock, S. / Fox, B. / Dore, M. / Labelle, M. / Sudom, A. / Johnstone, S. / Liu, J. / Walker, N.P. / Chai, A. / Siegler, K. / Li, Y. / Coward, P.
External linksBioorg. Med. Chem. Lett. / PubMed:19464171
MethodsX-ray diffraction
Resolution2 - 2.1 Å
Structure data

PDB-3gz9:
Crystal Structure of Peroxisome Proliferator-Activated Receptor Delta (PPARd) in Complex with a Full Agonist
Method: X-RAY DIFFRACTION / Resolution: 2 Å

PDB-3h0a:
Crystal Structure of Peroxisome Proliferator-Activated Receptor Gamma (PPARg) and Retinoic Acid Receptor Alpha (RXRa) in Complex with 9-cis Retinoic Acid, Co-activator Peptide, and a Partial Agonist
Method: X-RAY DIFFRACTION / Resolution: 2.1 Å

Chemicals

ChemComp-B7G:
heptyl beta-D-glucopyranoside

ChemComp-D32:
(2,3-dimethyl-4-{[2-(prop-2-yn-1-yloxy)-4-{[4-(trifluoromethyl)phenoxy]methyl}phenyl]sulfanyl}phenoxy)acetic acid

ChemComp-HOH:
WATER

ChemComp-9RA:
4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl]benzoic acid / anticancer, antineoplastic*YM

ChemComp-D30:
[(4-{[2-(pent-2-yn-1-yloxy)-4-{[4-(trifluoromethyl)phenoxy]methyl}phenyl]sulfanyl}-5,6,7,8-tetrahydronaphthalen-1-yl)oxy]acetic acid

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / PPAR / PPAR delta / nuclear receptor fold / transcription regulation / hormone / growth factor receptor / complex / Activator / Alternative splicing / DNA-binding / Metal-binding / Nucleus / Receptor / Zinc / Zinc-finger / Host-virus interaction / Isopeptide bond / Diabetes mellitus / Disease mutation / Obesity / Phosphoprotein / Acyltransferase / Proto-oncogene / Transferase

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