3OZ0

PPAR Delta in complex with azppard02

Summary for 3OZ0

• Entry DOI: 10.2210/pdb3oz0/pdb
• Descriptor: Peroxisome proliferator-activated receptor delta, [4-({(1S)-1-[(2,4-dichlorophenyl)carbamoyl]-1,3-dihydro-2H-isoindol-2-yl}methyl)-2-methylphenoxy]acetic acid (2 entities in total)
• Functional Keywords: transcription factor, transcription, nuclear receptor fold, transcription regulation, transcription-transcription regulator complex, transcription/transcription regulator
• Biological source: Homo sapiens (human)
• Cellular location: Nucleus: Q03181
• Total number of polymer chains: 1
• Total formula weight: 33166.19

Authors

Ogg, D. (deposition date: 2010-09-24, release date: 2011-01-19, Last modification date: 2023-09-06)

Primary citation

Luckhurst, C.A.,Stein, L.A.,Furber, M.,Webb, N.,Ratcliffe, M.J.,Allenby, G.,Botterell, S.,Tomlinson, W.,Martin, B.,Walding, A.
Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists
Bioorg.Med.Chem.Lett., 21:492-496, 2011

PubMed Abstract: Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor δ (PPARδ. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation, with upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) in human primary myotubes.

PubMed: 21094606
DOI: 10.1016/j.bmcl.2010.10.117

Experimental method

X-RAY DIFFRACTION (3 Å)