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TitlePhenoxyacetic acid PPARd partial agonists for the treatment of type 2 diabetes: synthesis, optimization, and in vivo efficacy
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 21, Page 2345-2350, Year 2011
Publish dateOct 27, 2010 (structure data deposition date)
AuthorsEvans, K.A. / Shearer, B.G. / Wisnoski, D.D. / Shi, D. / Sparks, S.M. / Sternbach, D.D. / Winegar, D.A. / Billin, A.N. / Britt, C. / Way, J.M. ...Evans, K.A. / Shearer, B.G. / Wisnoski, D.D. / Shi, D. / Sparks, S.M. / Sternbach, D.D. / Winegar, D.A. / Billin, A.N. / Britt, C. / Way, J.M. / Epperly, A.H. / Leesnitzer, L.M. / Merrihew, R.V. / Xu, R.X. / Lambert, M.H. / Jin, J.
External linksBioorg. Med. Chem. Lett. / PubMed:21414782
MethodsX-ray diffraction
Resolution2.4 Å
Structure data

PDB-3peq:
PPARd complexed with a phenoxyacetic acid partial agonist
Method: X-RAY DIFFRACTION / Resolution: 2.4 Å

Chemicals

ChemComp-3EQ:
[(4-{butyl[2-methyl-4'-(methylsulfanyl)biphenyl-3-yl]sulfamoyl}naphthalen-1-yl)oxy]acetic acid

ChemComp-JZR:
hexyl beta-D-glucopyranoside

ChemComp-IOD:
IODIDE ION

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION/TRANSCRIPTION agonist / PPAR nuclear receptor / TRANSCRIPTION-TRANSCRIPTION agonist complex

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