Shearer Barry G, Billin Andrew N
GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA.
Biochim Biophys Acta. 2007 Aug;1771(8):1082-93. doi: 10.1016/j.bbalip.2007.05.005. Epub 2007 Jun 2.
Agonists of PPARalpha and PPARgamma are currently approved for use in treating, respectively, dyslipidemia and type 2 diabetes. Agonists of PPARbeta/delta are currently in development by several pharmaceutical companies. Despite their therapeutic importance, there are dose limiting side effects associated with PPAR drug treatments, thus a new generation of safer PPAR drugs are being actively sought after. In this review we will discuss the side effects associated the PPARs, how the current drugs in clinical development were discovered and new concepts in how to screen for PPAR drugs.
PPARα和PPARγ激动剂目前已获批分别用于治疗血脂异常和2型糖尿病。PPARβ/δ激动剂目前正由几家制药公司进行研发。尽管它们具有治疗重要性,但PPAR药物治疗存在剂量限制副作用,因此正在积极寻求新一代更安全的PPAR药物。在本综述中,我们将讨论与PPAR相关的副作用、目前临床研发中的药物是如何被发现的,以及筛选PPAR药物的新概念。