2POB

PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709

Summary for 2POB

• Entry DOI: 10.2210/pdb2pob/pdb
• Descriptor: Peroxisome proliferator-activated receptor gamma, N-[(2S)-2-[(2-BENZOYLPHENYL)AMINO]-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]PHENYL}PROPYL]ACETAMIDE, GLYCEROL, ... (4 entities in total)
• Functional Keywords: pparg, nuclear receptor, ppar, gene regulation
• Biological source: Homo sapiens (human)
• Cellular location: Nucleus: P37231
• Total number of polymer chains: 2
• Total formula weight: 62854.04

Authors

Nolte, R.T. (deposition date: 2007-04-26, release date: 2008-03-18, Last modification date: 2024-04-03)

Primary citation

Trump, R.P.,Cobb, J.E.,Shearer, B.G.,Lambert, M.H.,Nolte, R.T.,Willson, T.M.,Buckholtz, R.G.,Zhao, S.M.,Leesnitzer, L.M.,Iannone, M.A.,Pearce, K.H.,Billin, A.N.,Hoekstra, W.J.
Cocrystal structure guided array synthesis of PPARgamma inverse agonists
BIOORG.MED.CHEM.LETT., 17:3916-3920, 2007

PubMed Abstract: 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.

PubMed: 17533125
DOI: 10.1016/j.bmcl.2007.04.111

Experimental method

X-RAY DIFFRACTION (2.3 Å)