Savkur Rajesh S, Miller Anne R
Eli Lilly and Company, Diabetes Research, Lilly Research Laboratories, Indianapolis, IN 46285, USA.
Expert Opin Investig Drugs. 2006 Jul;15(7):763-78. doi: 10.1517/13543784.15.7.763.
The tremendous increase in the global prevalence of Type 2 diabetes (T2D) and its conglomeration of metabolic disorders has dramatically intensified the search for innovative therapies to fight this emerging epidemic. Over the last decade, the family of nuclear receptors, especially the peroxisome proliferator-activated receptors (PPARs), has emerged as one of the most important drug targets aimed at combating the metabolic syndrome. Consequently, compounds that activate the PPARs have served as potential therapeutics for the treatment of T2D and the metabolic anomalies associated with this disorder. This review focuses on the currently marketed compounds and also describes the discovery and development of the next generation of PPAR ligands that are under investigation for the potential treatment of T2D and the metabolic syndrome.
2型糖尿病(T2D)在全球的患病率急剧上升及其代谢紊乱的聚集,极大地加剧了对对抗这一新兴流行病的创新疗法的探索。在过去十年中,核受体家族,尤其是过氧化物酶体增殖物激活受体(PPARs),已成为对抗代谢综合征的最重要药物靶点之一。因此,激活PPARs的化合物已成为治疗T2D及与此疾病相关的代谢异常的潜在疗法。本综述重点关注目前已上市的化合物,并描述了正在研究用于T2D和代谢综合征潜在治疗的下一代PPAR配体的发现与开发。