PPARA binds fibrates

The peroxisome proliferator-activated receptor alpha (PPARA) is a nuclear ligand-activated transcription factor that is a key regulator of fatty acid oxidation in the liver. Target genes of PPARA participate in fatty acid transport, fatty acid oxidation, triglyceride clearance, lipoprotein production, and cholesterol homeostasis. Its activation mediates lipid, glucose and amino acid homeostasis.<br><br>Fibrate drugs are derivatives of fibric acid which act as PPARA agonists and are widely used to lower triglycerides, LDL-cholesterol, total-cholesterol and apolipoprotein C3 (Grundy & Vega 1987, Clavey et al. 1999) while increasing HDL-cholesterol concentrations in serum. They are used to treat hypercholesterolemia, dyslipidemia and hypertriglyceridemia (Katsiki et al. 2013, Laufs et al. 2020). Fibrate drugs include gemfibrozil (De Filippis et al. 2011), bezafibrate (Inoue et al. 2002), cipofibrate (Quang et al. 2012), clofibrate (Henke et al. 1998) and fenofibrate (Caldwell 1989).

过氧化物酶体增殖激活受体α（PPARA）是一种核配体激活的转录因子，它是肝脏脂肪酸氧化的关键调节因子。PPARA的目标基因参与脂肪酸运输、脂肪酸氧化、甘油三酯清除、脂蛋白生成和胆固醇稳态的调节。其激活介导脂质、葡萄糖和氨基酸的稳态。纤维酸类药物为纤维酸的衍生物，作为PPARA激动剂，广泛用于降低甘油三酯、低密度脂蛋白胆固醇、总胆固醇和载脂蛋白C3（Grundy & Vega 1987，Clavey et al. 1999）水平，同时增加血清中的高密度脂蛋白胆固醇浓度。它们被用于治疗高胆固醇血症、血脂异常和高甘油三酯血症（Katsiki et al. 2013，Laufs et al. 2020）。纤维酸类药物包括吉非贝齐（De Filippis et al. 2011）、贝扎贝特（Inoue et al. 2002）、西波贝特（Quang et al. 2012）、氯贝丁酸（Henke et al. 1998）和苯贝特（Caldwell 1989）。