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首页> 外文期刊>Medicinal chemistry >Recent Updates on Peroxisome Proliferator-Activated Receptor Agonists for the Treatment of Metabolic Syndrome
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Recent Updates on Peroxisome Proliferator-Activated Receptor Agonists for the Treatment of Metabolic Syndrome

机译：过氧化物酶体增殖物激活的受体激动剂在代谢综合征治疗中的最新进展

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摘要

Metabolic syndrome is a disorder described by reduced insulin sensitivity, overweight, hyperlipidaemia, high blood pressure and myocardial disorders, mainly due to high fat diet and lack of physical activity. The peroxisome proliferator activated receptors (PPARs) are type II nuclear hormone receptors that regulate a number of processes in living systems, such as metabolism of carbohydrates and fatty acids, growth and differentiation of cell, and inflammatory reactions. Alpha, gamma and delta are the three distinct isoforms of PPAR. The stimulation of PPAR delta alters body's energy fuel preference from glucose to fat. The PPAR delta isoform is expressed ubiquitously in all tissues, especially in those tissues which involved in metabolism of lipids like adipose tissue, liver, kidney, and muscle. Currently, PPAR delta is an emerging therapeutic target for the pharmacological therapy of disorders associated with metabolic syndrome. Several PPAR delta selective agonists had been reported in last ten years, many of them had been advanced into the late phase of clinical trials such as Endurobol (GW501516). However, no PPAR delta agonists are yet approved for human use. The present work had been planned to cover wide variety of PPAR delta agonists reported till now along with their potential role to tackle various metabolic disorders. The present review has been planned to focus mainly the most popular PPAR delta agonists.
机译：代谢综合征是一种以胰岛素敏感性降低，超重，高血脂症，高血压和心肌疾病为特征的疾病，主要归因于高脂肪饮食和缺乏运动。过氧化物酶体增殖物激活受体（PPAR）是II型核激素受体，可调节生物系统中的许多过程，例如碳水化合物和脂肪酸的代谢，细胞的生长和分化以及炎症反应。 α，γ和δ是PPAR的三种不同的同工型。 PPARδ的刺激改变了人体从葡萄糖到脂肪的能源偏好。 PPARδ同工型在所有组织中普遍存在，特别是在那些涉及脂质代谢的组织中，例如脂肪组织，肝脏，肾脏和肌肉中普遍表达。当前，PPARδ是与代谢综合征相关的疾病的药物治疗的新兴治疗靶标。在过去的十年中，已经报道了几种PPARδ选择性激动剂，其中许多已经进入临床试验的后期阶段，例如Endurobol（GW501516）。但是，尚未批准将PPARδ激动剂用于人类。计划目前的工作以涵盖迄今为止报道的各种PPARδ激动剂及其在解决各种代谢异常中的潜在作用。目前的审查计划主要集中在最受欢迎的PPARδ激动剂上。

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