Nishizuka Makoto, Imagawa Masayoshi
Department of Molecular Biology, Graduate School of Pharmaceutical Sciences, Nagoya City University.
Nihon Rinsho. 2010 Feb;68(2):189-93.
Peroxisome proliferator-activated receptor gamma (PPARgamma) agonist such as thiazolidinedione (TZD) has important roles in inflammation and cancer in addition to the control of energy conservation, adipocyte differentiation and insulin sensitivity. PPARgamma is a ligand-activated nuclear receptor. In the absence of ligand, the transcriptional activity of PPARgamma is suppressed through the association with N-CoR/SMRT and histone deacetylases. Upon binding of ligand to PPARgamma, PPARgamma binds several coactivators and regulates the expression of its target genes in various tissues. To understand various effects of TZD, we summarize the transcriptional control by PPARgamma focused on coactivators and target genes regulated by PPARgamma.
过氧化物酶体增殖物激活受体γ(PPARγ)激动剂,如噻唑烷二酮(TZD),除了在能量储存、脂肪细胞分化和胰岛素敏感性控制方面发挥作用外,在炎症和癌症中也具有重要作用。PPARγ是一种配体激活的核受体。在没有配体的情况下,PPARγ的转录活性通过与N-CoR/SMRT和组蛋白脱乙酰酶结合而受到抑制。当配体与PPARγ结合后,PPARγ会结合多种共激活因子,并调节其在各种组织中的靶基因表达。为了了解TZD的各种作用,我们总结了PPARγ的转录调控,重点关注由PPARγ调控的共激活因子和靶基因。