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PPARdelta in humans: genetic and pharmacological evidence for a significant metabolic function.

机译:人体内的PPARdelta:具有重要的代谢功能的遗传和药理证据。

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PURPOSE OF REVIEW: Abundant data in rodents suggest an important role for peroxisomal proliferators-activated receptor-delta (PPARdelta) in regulating skeletal muscle fatty acid oxidation and this has consequences for lipid and lipoprotein metabolism. Considerably less is known in humans and this review will focus on evidence derived from studies of the PPARD gene and pharmacological use of specific PPARdelta agonists. RECENT FINDINGS: Genetic association studies of single-nucleotide polymorphisms in the PPARD gene have only provided negative or conflicting evidence for gross phenotypes such as obesity, hyperlipidaemia and type 2 diabetes. This does not exclude more subtle effects in skeletal muscle metabolic function, but studies of this type need replication. A couple of recent studies using the specific PPARdelta agonist GW501516 suggest potent hypolipidaemic actions, presumably caused by enhanced fat oxidation in skeletal muscle. SUMMARY: Considering the hypolipidaemic effect in humans by PPARdelta agonists, long-term studies are needed to confirm efficacy and safety.
机译:审查的目的:啮齿动物的大量数据表明过氧化物酶体增殖物激活的受体-δ(PPARdelta)在调节骨骼肌脂肪酸氧化中起重要作用,这对脂质和脂蛋白代谢具有影响。在人类中所知甚少,本文将重点研究PPARD基因的研究以及特定PPARδ激动剂的药理用途。最近的发现:PPARD基因中单核苷酸多态性的遗传关联研究仅为肥胖,高脂血症和2型糖尿病等总体表型提供了阴性或相互矛盾的证据。这并不排除对骨骼肌代谢功能的更微妙的影响,但是这种类型的研究需要复制。最近有几项使用特定的PPARδ激动剂GW501516的研究表明,强效降血脂作用可能是骨骼肌脂肪氧化增强所致。摘要:考虑到PPARdelta激动剂对人体的降血脂作用,需要长期研究以确认疗效和安全性。

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