Departamento Ciencias Biomédicas, Facultad Ciencias de la Salud, Universidad de Talca, Chile.
Mediators Inflamm. 2013;2013:549627. doi: 10.1155/2013/549627. Epub 2013 May 27.
Metabolic syndrome is estimated to affect more than one in five adults, and its prevalence is growing in the adult and pediatric populations. The most widely recognized metabolic risk factors are atherogenic dyslipidemia, elevated blood pressure, and elevated plasma glucose. Individuals with these characteristics commonly manifest a prothrombotic state and a proinflammatory state as well. Peroxisome proliferator-activated receptors (PPARs) may serve as potential therapeutic targets for treating the metabolic syndrome and its related risk factors. The PPARs are transcriptional factors belonging to the ligand-activated nuclear receptor superfamily. So far, three isoforms of PPARs have been identified, namely, PPAR- α, PPAR-β/δ, and PPAR-γ. Various endogenous and exogenous ligands of PPARs have been identified. PPAR- α and PPAR- γ are mainly involved in regulating lipid metabolism, insulin sensitivity, and glucose homeostasis, and their agonists are used in the treatment of hyperlipidemia and T2DM. Whereas PPAR- β / δ function is to regulate lipid metabolism, glucose homeostasis, anti-inflammation, and fatty acid oxidation and its agonists are used in the treatment of metabolic syndrome and cardiovascular diseases. This review mainly focuses on the biological role of PPARs in gene regulation and metabolic diseases, with particular focus on the therapeutic potential of PPAR modulators in the treatment of thrombosis.
代谢综合征估计影响超过五分之一的成年人，且其在成年和儿科人群中的患病率正在增长。最广泛认可的代谢危险因素是动脉粥样硬化性血脂异常、血压升高和血浆葡萄糖升高。具有这些特征的个体通常表现出促血栓形成状态和促炎状态。过氧化物酶体增殖物激活受体 (PPARs) 可能是治疗代谢综合征及其相关危险因素的潜在治疗靶点。PPARs 是属于配体激活核受体超家族的转录因子。迄今为止，已经鉴定出三种 PPAR 异构体，即 PPAR-α、PPAR-β/δ 和 PPAR-γ。已经鉴定出各种内源性和外源性的 PPARs 配体。PPAR-α 和 PPAR-γ 主要参与调节脂质代谢、胰岛素敏感性和葡萄糖稳态，其激动剂用于治疗高脂血症和 T2DM。而 PPAR-β/δ 的功能是调节脂质代谢、葡萄糖稳态、抗炎和脂肪酸氧化，其激动剂用于治疗代谢综合征和心血管疾病。本综述主要关注 PPARs 在基因调节和代谢疾病中的生物学作用，特别关注 PPAR 调节剂在治疗血栓形成方面的治疗潜力。
