Fibrates, Glitazones, and Peroxisome Proliferator-Activated Receptors
Fibrates, Glitazones, and Peroxisome Proliferator-Activated Receptors
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DOI：
10.1161/atvbaha.108.179689
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发表时间：
2010-05-01
影响因子：
8.7
通讯作者：
Staels, Bart
中科院分区：
文献类型：
--
作者：
Lalloyer, Fanny;Staels, Bart
a几十年前，贝特类药物被批准用于治疗血脂异常，而噻唑烷二酮类药物在动物模型中被筛选用于改善葡萄糖稳态，随后被开发用于治疗2型糖尿病。最近，这些药物被发现通过过氧化物酶体增殖激活受体，控制脂质代谢和葡萄糖稳态的核受体起作用。从这个历史的角度来看，我们讨论了过氧化物酶体增殖物激活受体的发现历史，从它们的激动剂的临床发展到这些受体的后续发现及其作用机制，最终唤起了选择性过氧化物酶体增殖物激活受体调节剂未来发展的靶向药理学可能性。（中华动脉血管杂志，2010;30:894-899）
a Several decades ago, fibrates were approved for the treatment of dyslipidemia, whereas thiazolidinediones were screened in animal models to improve glucose homeostasis and were subsequently developed for the treatment of type 2 diabetes mellitus. Relatively recently, these drugs were found to act via peroxisome proliferator-activated receptors, nuclear receptors that control lipid metabolism and glucose homeostasis. In this historical perspective, we discuss the history of discovery of the peroxisome proliferator-activated receptors, from the clinical development of their agonists to the subsequent discovery of these receptors and their mechanisms of action, to finally evoke possibilities of targeted pharmacology for future development of selective peroxisome proliferator-activated receptor modulators. (Arterioscler Thromb Vasc Biol. 2010; 30: 894-899.)