Dubois Vanessa, Eeckhoute Jérôme, Lefebvre Philippe, Staels Bart
J Clin Invest. 2017 Apr 3;127(4):1202-1214. doi: 10.1172/JCI88894.
Peroxisome proliferator-activated receptors (PPARs) regulate energy metabolism and hence are therapeutic targets in metabolic diseases such as type 2 diabetes and non-alcoholic fatty liver disease. While they share anti-inflammatory activities, the PPAR isotypes distinguish themselves by differential actions on lipid and glucose homeostasis. In this Review we discuss the complementary and distinct metabolic effects of the PPAR isotypes together with the underlying cellular and molecular mechanisms, as well as the synthetic PPAR ligands that are used in the clinic or under development. We highlight the potential of new PPAR ligands with improved efficacy and safety profiles in the treatment of complex metabolic disorders.
过氧化物酶体增殖物激活受体(PPARs)调节能量代谢,因此是2型糖尿病和非酒精性脂肪性肝病等代谢性疾病的治疗靶点。虽然它们具有共同的抗炎活性,但PPAR亚型在对脂质和葡萄糖稳态的不同作用方面有所区别。在本综述中,我们讨论了PPAR亚型的互补和独特的代谢作用及其潜在的细胞和分子机制,以及临床使用或正在研发的合成PPAR配体。我们强调了具有改善疗效和安全性的新型PPAR配体在治疗复杂代谢紊乱方面的潜力。