胆固醇逆向转运过程中新靶点及其药物的研究进展

Progress in new drugs targeting reverse cholesterol transport

血浆高密度脂蛋白胆固醇(HDLC)拮抗动脉粥样硬化(AS)的最主要机制在于参与胆固醇逆向转运(RCT)过程。近年来,将RCT过程中几个重要蛋白质和酶类,包括apoAⅠ,ABCA1,CETP等作为新的用药靶点进行了药物干预的尝试,在调节血脂和预防AS等方面取得了良好的效果,开创了治疗该类疾病的新局面,对下一步的疾病治疗具有重要的指导作用。

Numerous epidemiologic studies have shown that there is a strong inverse relationship between highdensity lipoprotein cholesterol levels and artherosclerosis. The first atheroprotective mechanism of HDL is the RCT （ reverse cholesterol transport）. Recently, considerable pharmacological trials have focused on targeting critical proteins and enzymes in RCT including apoA Ⅰ, ATP binding cassette transporter A1 and cholesteryl ester transport protein etc. A number of new drugs have demonstrated conspicuous protective effects on artherosclerosis. Therefore RCT will become an attractive target for prevention and cure of dyslipidamia and artherosclerosis.