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胆固醇酯转移蛋白(CETP)是胆固醇逆转运(RCT)循环中协调脂质转运的重要蛋白。CETP调控胆固醇酯和甘油三酯在高密度脂蛋白、低密度脂蛋白和极低密度脂蛋白之间的转运,在高密度脂蛋白代谢中起核心作用。抑制CETP活性可以有效提高体内高密度脂蛋白水平(同时降低低密度脂蛋白水平)从而可以预防心血管疾病的发生,因此CETP是一个非常具有开发前景的潜在调血脂药物作用靶标。本文对新降脂靶点CETP及目前CETP抑制剂的最新研究现状进行综述。
Cholesteryl ester transfer protein (CETP) is an important protein that mediates lipid transport in the cholesterol reverse transport (RCT) cycle. CETP regulates the transport of cholesterol esters and triglycerides between high-density lipoproteins, low-density lipoproteins and very-low-density lipoproteins and plays a central role in high-density lipoprotein metabolism. Inhibition of CETP activity can effectively increase high-density lipoprotein (HDL-C) levels in vivo and reduce the level of LDL, thereby preventing cardiovascular diseases. Therefore, CETP is a promising target for lipid-lowering drugs. This review summarizes the latest research status of new lipid-lowering target CETP and current CETP inhibitors.