Center for Cardiovascular Diseases, College of Pharmacy and Health Sciences, Texas Southern University, Houston, Texas 77004, USA.
Clin Exp Hypertens. 2011;33(5):287-93. doi: 10.3109/10641963.2010.531845. Epub 2011 Jul 1.
Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors belonging to the nuclear receptor superfamily that undergo transactivation or transrepression by distinct mechanisms leading to induction or repression of expression of target genes. The PPAR family consists of three isoforms, α, γ, and ß/δ, which share similar structural organization, possess distinct functions, and vary in their ligand affinity, expression, and activity in different metabolic pathways in different tissues. PPARs are involved in many functions especially those involved in the regulation of vascular tone, inflammation and energy homeostasis and therefore represent important targets for hypertension, obesity, obesity-induced inflammation, and metabolic syndrome in general. PPARs may influence the inflammatory response either by direct transcriptional downregulation of proinflammatory genes via mechanisms involving transrepression, or indirectly via their transcriptional effects on lipid metabolism. On account of their pleiotropic effects, they are now known to be active participants in many disease conditions and they represent potent targets for the development of therapy of a wide array of diseases.
过氧化物酶体增殖物激活受体 (PPARs) 是配体激活的转录因子，属于核受体超家族，通过不同的机制进行转录激活或转录抑制，从而诱导或抑制靶基因的表达。PPAR 家族由三个亚型，α、γ 和 ß/δ 组成，它们具有相似的结构组织，具有不同的功能，在不同组织的不同代谢途径中对配体的亲和力、表达和活性也不同。PPARs 参与许多功能，特别是涉及血管张力、炎症和能量平衡的调节，因此是高血压、肥胖、肥胖引起的炎症和代谢综合征等一般疾病的重要靶点。PPARs 可以通过涉及转录抑制的机制，直接转录下调促炎基因，或者通过对脂质代谢的转录效应间接影响炎症反应。由于其多效性作用，它们现在被认为是许多疾病状态的积极参与者，并且是开发广泛疾病治疗方法的有效靶点。
