3oz0

PPAR Delta in complex with azppard02PPAR Delta in complex with azppard02

Structural highlights

3oz0 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Gene:	PPARD, NR1C2, PPARB (Homo sapiens)
Resources:	FirstGlance, OCA, RCSB, PDBsum

Publication Abstract from PubMed

Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor delta (PPARdelta. 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.

Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARdelta agonists.,Luckhurst CA, Stein LA, Furber M, Webb N, Ratcliffe MJ, Allenby G, Botterell S, Tomlinson W, Martin B, Walding A Bioorg Med Chem Lett. 2011 Jan 1;21(1):492-6. Epub 2010 Oct 27. PMID:21094606^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Luckhurst CA, Stein LA, Furber M, Webb N, Ratcliffe MJ, Allenby G, Botterell S, Tomlinson W, Martin B, Walding A. Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARdelta agonists. Bioorg Med Chem Lett. 2011 Jan 1;21(1):492-6. Epub 2010 Oct 27. PMID:21094606 doi:10.1016/j.bmcl.2010.10.117

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OCA

[1] Luckhurst CA, Stein LA, Furber M, Webb N, Ratcliffe MJ, Allenby G, Botterell S, Tomlinson W, Martin B, Walding A. Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARdelta agonists. Bioorg Med Chem Lett. 2011 Jan 1;21(1):492-6. Epub 2010 Oct 27. PMID:21094606 doi:10.1016/j.bmcl.2010.10.117

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