Yamagishi Sho-ichi
Department of Pathophysiology and Therapeutics of Diabetic Vascular Complications, Kurume University School of Medicine.
Nihon Rinsho. 2010 Feb;68(2):307-11.
Peroxisome proliferator-activated receptor-gamma (PPARgamma) is a nuclear receptor protein. It functions as a master transcriptional factor that promotes differentiation of preadipocytes by activating adipose-specific gene expression. Recently, PPARgamma activity has been shown to influence the gene expression involved in carbohydrate and lipid metabolism. Indeed, pioglitazone and rosiglitazone, ligands for PPARgamma, improve insulin resistance in diabetic patients, and now become one of the most popular anti-diabetic drugs in the developed countries. Moreover, there is accumulating data that PPARgamma ligands exert anti-inflammatory, anti-oxidative and anti-proliferative effects on vascular wall cells. These observations suggest that PPARgamma agonist may have atheroprotective properties as well through its pleiotropic effects. In this paper, we review the clinical utility of PPARgamma agonist in the treatment of cardiovascular disease.
过氧化物酶体增殖物激活受体γ(PPARγ)是一种核受体蛋白。它作为主要转录因子发挥作用,通过激活脂肪特异性基因表达促进前脂肪细胞分化。最近,已表明PPARγ活性会影响参与碳水化合物和脂质代谢的基因表达。事实上,吡格列酮和罗格列酮作为PPARγ的配体,可改善糖尿病患者的胰岛素抵抗,现已成为发达国家最常用的抗糖尿病药物之一。此外,越来越多的数据表明PPARγ配体对血管壁细胞具有抗炎、抗氧化和抗增殖作用。这些观察结果表明,PPARγ激动剂可能也因其多效性作用而具有动脉粥样硬化保护特性。在本文中,我们综述了PPARγ激动剂在心血管疾病治疗中的临床应用。