Grimaldi Paul André
Inserm U636, Centre de Biochimie, UFR Sciences, Université de Nice-Sophia Antipolis, Parc Valrose, 06108 Nice, France.
Biochimie. 2005 Jan;87(1):5-8. doi: 10.1016/j.biochi.2004.11.009.
Peroxisome proliferator-activated receptors (PPARs) are transcription factors involved in both developmental and metabolic functions. There are activated by fatty acids, fatty acid metabolites, and synthetic compounds marketed for their lipid-lowering and antidiabetic actions. It was clearly established that activation of PPAR alpha and PPAR gamma, by fibrates and thiazolidinediones, respectively, impair metabolic disorders. The implication of the third member of the PPAR family, PPAR delta, remained evasive until recently. These past few years, it has been demonstrated that treatment with PPAR delta agonists normalizes blood lipids, reduces insulin resistance and adiposity in rodent and primate. Utilization of both cellular and animal models revealed that the nuclear receptor plays a central role in the control of fatty acid burning in adipose tissue and skeletal muscle. Furthermore, PPAR delta appeared to be important for adaptive response of skeletal muscle to environmental changes, such as physical exercise.
过氧化物酶体增殖物激活受体（PPARs）是参与发育和代谢功能的转录因子。它们被脂肪酸、脂肪酸代谢产物以及因其降脂和抗糖尿病作用而上市的合成化合物激活。已明确证实，贝特类药物和噻唑烷二酮类药物分别激活PPARα和PPARγ可改善代谢紊乱。直到最近，PPAR家族的第三个成员PPARδ的作用仍不明确。在过去几年中，已证明用PPARδ激动剂治疗可使啮齿动物和灵长类动物的血脂正常化，降低胰岛素抵抗和肥胖。细胞和动物模型的研究表明，这种核受体在控制脂肪组织和骨骼肌中的脂肪酸燃烧方面起着核心作用。此外，PPARδ对于骨骼肌对环境变化（如体育锻炼）的适应性反应似乎也很重要。
