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Details on Person Peroxisome proliferator-activated receptor gamma (PPARG) is ...

Class:IdSummation:9733254
_displayNamePeroxisome proliferator-activated receptor gamma (PPARG) is ...
_timestamp2021-06-02 09:53:56
created[InstanceEdit:9733253] Jassal, Bijay, 2021-06-02
literatureReference[LiteratureReference:9733269] Liver enzyme monitoring in patients treated with troglitazone
[LiteratureReference:9733258] Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission
textPeroxisome 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 Troglitazone was withdrawn in 2000 due to risk of hepatotoxicity (Graham et al. 2001) but has since been extensively studied using a variety of in vivo, in vitro and computational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).
(summation)[Reaction:9732629] PPARG binds PPARG agonists [Homo sapiens]
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