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首页> 外文期刊>European Journal of Pharmacology: An International Journal >A step ahead of PPAR gamma full agonists to PPAR gamma partial agonists: Therapeutic perspectives in the management of diabetic insulin resistance
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A step ahead of PPAR gamma full agonists to PPAR gamma partial agonists: Therapeutic perspectives in the management of diabetic insulin resistance

机译：从PPARγ完全激动剂到PPARγ局部激动剂迈出的一步：糖尿病胰岛素抵抗治疗的治疗观点

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Described since long as a member of the nuclear receptor superfamily, peroxisome proliferator-activated receptors (PPARs) regulate the gene expression of proteins involved in glucose and lipid metabolism. PPARs indeed regulate several physiologic processes, including lipid homeostasis, adipogenesis, inflammation, and wound healing. PPARs bind natural or synthetic PPAR ligands can function as cellular sensors to regulate the gene transcription. Dyslipidemia, and type 2 diabetes mellitus (T2DM) with insulin resistance are treated using agonists of PPAR alpha and PPAR gamma, respectively. The PPAR gamma is a key regulator of insulin sensitization and glucose metabolism, and therefore is considered as an imperative pharmacological target to combat diabetic metabolic disease and insulin resistance. Of note, currently available PPAR gamma full agonists like rosiglitazone display serious adverse effects such as fluid retention/ oedema, weight gain, and increased incidence of cardiovascular events. On the other hand, PPAR gamma partial agonists are being suggested to devoid or having less incidence of these undesirable events, and are under developmental stages. Current research is on the way for the development of novel PPAR gamma partial agonists with enhanced therapeutic efficacy and reduced adverse effects. This review sheds lights on the current status of development of PPAR gamma partial agonists, for the management of T2DM, having comparatively less or no adverse effects to that of PPARy full agonists. (C) 2015 Elsevier B.V. All rights reserved.
机译：自从作为核受体超家族的成员被描述以来，过氧化物酶体增殖物激活的受体（PPAR）调节参与葡萄糖和脂质代谢的蛋白质的基因表达。 PPAR确实可调节多种生理过程，包括脂质稳态，脂肪形成，炎症和伤口愈合。 PPAR结合天然或合成的PPAR配体可充当细胞传感器来调节基因转录。血脂异常和具有胰岛素抵抗的2型糖尿病（T2DM）分别使用PPARα和PPARγ激动剂进行治疗。 PPARγ是胰岛素增敏和葡萄糖代谢的关键调节剂，因此被认为是抵抗糖尿病代谢疾病和胰岛素抵抗的必要药理学靶标。值得注意的是，目前可用的PPARγ完全激动剂（如罗格列酮）显示出严重的不良反应，例如体液retention留/水肿，体重增加和心血管事件发生率增加。另一方面，建议PPARγ部分激动剂避免或较少发生这些不良事件，并且处于发育阶段。当前的研究正在开发具有增强的治疗功效和减少的副作用的新型PPARγ部分激动剂。这篇综述揭示了PPARγ部分激动剂的发展现状，用于T2DM的管理，对PPARγ完全激动剂的副作用相对较小或没有。 （C）2015 Elsevier B.V.保留所有权利。

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