PPARG binds PPARG agonists

Stable Identifier
Reaction [binding]
Homo sapiens
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Peroxisome proliferator-activated receptor gamma (PPARG) is expressed mainly in fat tissue, where it regulates genes involved in fat cell (adipocyte) differentiation, fatty acid uptake and storage, and glucose uptake. PPARG is a nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, PPARG binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes. PPARG can regulate peroxisomal fatty acid beta-oxidation, adipocyte differentiation and glucose homeostasis.

Thiazolidinediones (TZDs, glitazones) are a family of drugs acting as insulin sensitizers and are only approved for the treatment of type 2 diabetes mellitus (T2DM). TZDs are PPARG agonists and act via PPARG to make cells more responsive to insulin. TZDs used to manage T2DM are rosiglitazone (Henke et al. 1998, Young et al. 1998), pioglitazone (Sakamoto et al. 2000) and troglitazone (Henke et al. 1998). Troglitazone was withdrawn in 2000 due to risk of hepatotoxicity (Graham et al. 2001) but has since been extensively studied using a variety of in vivo, in vitro and computational methods (Kassahun et al. 2001).
Literature References
PubMed ID Title Journal Year
9836620 N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents

Collins, JL, Brackeen, MF, Kliewer, SA, Lehmann, JM, Blanchard, SG, Brown, KK, Leesnitzer, LM, Henke, BR, Hull-Ryde, EA, Miller, JF, Kaldor, I, Willson, TM, Szewczyk, JR, Orband-Miller, LA, Cobb, JE, Harrington, WW, Oliver, W, Mook, RA, Plunket, KD, Noble, SA, Lenhard, JM, Parks, DJ, Lake, DH, Hashim, MA

J Med Chem 1998
9454824 Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma

Chapman, H, Kallender, H, Coyle, PJ, Murphy, GJ, Clapham, JC, Hindley, RM, Cantello, BC, Mossakowska, D, Young, PW, Holder, JC, Buckle, DR, Lawrie, KW, Roxbee Cox, L, Latter, AJ, Haigh, D, Smith, SA

J Pharmacol Exp Ther 1998
11095972 Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone

Odaka, H, Sawada, H, Moriyama, S, Sugiyama, Y, Momose, Y, Kimura, H, Sakamoto, J

Biochem Biophys Res Commun 2000
Orthologous Events
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