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多靶点过氧化物酶体增殖物激活受体 γ 激动剂作为代谢综合征的创新性调节剂。

Multitarget PPARγ agonists as innovative modulators of the metabolic syndrome.

机构信息

Department of Pharmacy, University of Chieti "G. d.Annunzio", Via Dei Vestini, 31, 66100, Chieti, Italy.

Department of Pharmacy, University of Chieti "G. d.Annunzio", Via Dei Vestini, 31, 66100, Chieti, Italy.

出版信息

Eur J Med Chem. 2019 Jul 1;173:261-273. doi: 10.1016/j.ejmech.2019.04.030. Epub 2019 Apr 13.

Abstract

A multitarget pharmacologic approach could be advantageous for the therapy of metabolic multiple diseases, such as the metabolic syndrome, which is characterized by metabolic abnormalities associated with diabetes, obesity, hypertension, and increased cardiovascular risk. PPAR receptors play a critical role in metabolic disorders, affecting glucose and lipid metabolism. Drugs simultaneously targeting PPAR and other validated metabolic targets, represent a promising multitarget approach to combine antihyperglycemic, antihyperlipidemic, and antihypertensive effects. This review offers a survey of recently developed multitarget PPARγ agonists as antidiabetic and antihypertensive drugs.

摘要

多靶点药物治疗策略可能有利于治疗多种代谢性疾病,如代谢综合征。代谢综合征的特征是与糖尿病、肥胖症、高血压和心血管风险增加相关的代谢异常。过氧化物酶体增殖物激活受体(PPAR)在代谢紊乱中发挥着关键作用,影响葡萄糖和脂质代谢。同时针对 PPAR 和其他已验证的代谢靶点的药物代表了一种有前途的多靶点方法,可以结合抗高血糖、抗高血脂和抗高血压作用。本综述概述了最近开发的多靶点 PPARγ 激动剂作为抗糖尿病和抗高血压药物。

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