2pob | pdb_00002pob
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| 2pob, resolution 2.30Å | |||||||||||||
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| Sites: | AC1 and AC2 | ||||||||||||
| Ligands: | GW4 and GOL | ||||||||||||
| Gene: | PPARG, NR1C3 (Homo sapiens) | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709
Overview
PPARgamma-activating thiazolidinediones and carboxylic acids such as farglitazar exert their anti-diabetic effects in part in PPARgamma rich adipose. Both pro- and anti-adipogenic PPARgamma ligands promote glucose and lipid lowering in animal models of diabetes. Herein, we disclose representatives of an array of 160 farglitazar analogues with atypical inverse agonism of PPARgamma in mature adipocytes.
About this Structure
2POB is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Co-crystal structure guided array synthesis of PPARgamma inverse agonists., Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ, Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. Epub 2007 May 18. PMID:17533125
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