Peroxisome proliferator-activated receptor-α (PPARα), PPARδ and PPARγ are transcription factors that regulate gene expression following ligand activation. PPARα increases cellular fatty acid uptake, esterification and trafficking, and regulates lipoprotein metabolism genes. PPARδ stimulates lipid and glucose utilization by increasing mitochondrial function and fatty acid desaturation pathways. By contrast, PPARγ promotes fatty acid uptake, triglyceride formation and storage in lipid droplets, thereby increasing insulin sensitivity and glucose metabolism. PPARs also exert antiatherogenic and anti-inflammatory effects on the vascular wall and immune cells. Clinically, PPARγ activation by glitazones and PPARα activation by fibrates reduce insulin resistance and dyslipidaemia, respectively. PPARs are also physiological master switches in the heart, steering cardiac energy metabolism in cardiomyocytes, thereby affecting pathological heart failure and diabetic cardiomyopathy. Novel PPAR agonists in clinical development are providing new opportunities in the management of metabolic and cardiovascular diseases.

过氧化物酶体增殖物激活受体-α (PPARα)、PPARδ 和 PPARγ 是配体激活后调节基因表达的转录因子。PPARα 增加细胞脂肪酸的摄取、酯化和运输，并调节脂蛋白代谢基因。PPARδ 通过增加线粒体功能和脂肪酸去饱和途径来刺激脂质和葡萄糖的利用。相比之下，PPARγ促进脂肪酸的摄取、甘油三酯的形成和脂滴的储存，从而增加胰岛素敏感性和葡萄糖代谢。PPAR 还对血管壁和免疫细胞发挥抗动脉粥样硬化和抗炎作用。临床上，格列酮激活 PPARγ 和贝特类激活 PPARα 分别可降低胰岛素抵抗和血脂异常。PPARs还是心脏的生理总开关，控制心肌细胞的心脏能量代谢，从而影响病理性心力衰竭和糖尿病心肌病。临床开发中的新型 PPAR 激动剂为代谢和心血管疾病的治疗提供了新的机会。