Bishop-Bailey D
Vascular Biology Center, Department of Physiology, University of Connecticut Health Center, 263 Farmington Avenue, Farmington, Connecticut, CT 06030-3505, USA.
Br J Pharmacol. 2000 Mar;129(5):823-34. doi: 10.1038/sj.bjp.0703149.
Peroxisome proliferator-activated receptor (PPAR)s are a family of three nuclear hormone receptors, PPARalpha, -delta, and -gamma, which are members of the steriod receptor superfamily. The first member of the family (PPARalpha) was originally discovered as the mediator by which a number of xenobiotic drugs cause peroxisome proliferation in the liver. Defined functions for all these receptors, until recently, mainly concerned their ability to regulate energy balance, with PPARalpha being involved in beta-oxidation pathways, and PPARgamma in the differentiation of adipocytes. Little is known about the functions of PPARdelta, though it is the most ubiquitously expressed. Since their discovery, PPARs have been shown to be expressed in monocytes/macrophages, the heart, vascular smooth muscle cells, endothelial cells, and in atherosclerotic lesions. Furthermore, PPARs can be activated by a vast number of compounds including synthetic drugs, of the clofibrate, and anti-diabetic thiazoldinedione classes, polyunsaturated fatty acids, and a number of eicosanoids, including prostaglandins, lipoxygenase products, and oxidized low density lipoprotein. This review will aim to introduce the field of PPAR nuclear hormone receptors, and discuss the discovery and actions of PPARs in the cardiovascular system, as well as the source of potential ligands.
过氧化物酶体增殖物激活受体(PPAR)是由三种核激素受体组成的家族,即PPARα、-δ和-γ,它们是类固醇受体超家族的成员。该家族的第一个成员(PPARα)最初被发现是许多外源性药物导致肝脏中过氧化物酶体增殖的介质。直到最近,所有这些受体的明确功能主要涉及其调节能量平衡的能力,PPARα参与β-氧化途径,PPARγ参与脂肪细胞的分化。尽管PPARδ是表达最广泛的,但对其功能了解甚少。自发现以来,PPAR已被证明在单核细胞/巨噬细胞、心脏、血管平滑肌细胞、内皮细胞以及动脉粥样硬化病变中表达。此外,PPAR可被大量化合物激活,包括合成药物,如氯贝特类和抗糖尿病噻唑烷二酮类、多不饱和脂肪酸以及一些类花生酸,包括前列腺素、脂氧合酶产物和氧化型低密度脂蛋白。本综述旨在介绍PPAR核激素受体领域,并讨论PPAR在心血管系统中的发现和作用,以及潜在配体的来源。