Title:Role of Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) in Different Disease States: Recent Updates
Volume: 28
Issue: 16
关键词:
过氧化物酶体增殖物激活受体、PPAR γ、泛 PPAR 配体、糖尿病、癌症、膀胱肿瘤。
摘要: Peroxisome proliferator-activated receptor (PPAR), a ligand dependant transcription
factor, is a member of the nuclear receptor superfamily. PPAR exists in three isoforms
i.e. PPAR alpha (PPARα), PPAR beta (PPARβ), and PPAR gamma (PPARγ). These are
multi-functional transcription factors and help in regulating inflammation, type 2 diabetes,
lipid concentration in the body, metastasis, and tumor growth or angiogenesis. Activation of
PPARγ causes inhibition of growth of cultured human breast, gastric, lung, prostate, and other
cancer cells. PPARγ is mainly involved in fatty acid storage, glucose metabolism, and homeostasis
and adipogenesis regulation. A large number of natural and synthetic ligands bind to
PPARγ and modulate its activity. Ligands such as thiazolidinedione, troglitazone, rosiglitazone,
pioglitazone effectively bind to PPARγ; however, most of these were found to display
severe side effects such as hepatotoxicity, weight gain, cardiovascular complications and
bladder tumor. Now the focus is shifted towards the development of dual-acting or pan PPAR
ligands. The current review article describes the functions and role of PPARγ in various disease
states. In addition, recently reported PPARγ ligands and pan PPAR ligands were discussed
in detail. It is envisaged that the present review article may help in the development of
potent PPAR ligands with no or minimal side effects.
