调脂药物的作用靶点

Targets of anti-hyperlipidemia drugs

血脂异常是动脉粥样硬化、冠心病等心血管疾病的重要危险因素,调脂药物治疗的主要目标是降低血浆低密度脂蛋白,升高高密度脂蛋白。尼曼-匹克C1型类似蛋白1(NPC1L1),胆固醇酰基转移酶(ACAT),三磷酸腺苷结合盒转运体G5和G8(ABCG5/G8),微粒体三酰甘油转运蛋白(MTP),单酰基甘油酰基转移酶(MAGT),二酰基甘油酰基转移酶(DAGT),过氧化物酶体增生激活型受体(PPAR),法尼醇X受体(FXR),前蛋白转化酶枯草溶菌素9(PCSK9)等是参与血脂代谢的重要蛋白,也是调脂药物作用相关的靶点,在调脂药物的开发和临床用药选择上具有重要参考价值。

Hyperlipidemia is one of the most important risk factors for atherosclerosis, coronary heart disease and other cardiovascular diseases. It is the main effect of lipid-lowering drugs to reduce the plasma low-density lipoprotein or to enhance high-density lipoprotein. Niemann-Pick C1 like 1 protein （NPC ILl）, acyl-coenzyme A： cholesterol acyltransferases （ACAT）, ATP binding cassette transporter G member 5 and member 8 （ABCGS/G8）, microsomal triglyceride transfer protein （MTP）, monoacylglycerol acyltransferase, diacylglycerol acyltransferases （MAGT）, peroxisome proliferator-activated receptor （PPAR）, farnesoid X receptor （FXR）, and proprotein convertase subtilisin/kexin type 9 （PCSK9） play key roles in the metabolism of lipid, which are regarded as the targets of anti-hyperlipidemia drugs and evidence for clinic choice of lipid-lowering drugs. These proteins are considered as breakthrough points for new lipid-lowering drug development.