ApoA-Ⅰ模拟肽抗动脉粥样硬化的研究进展  

Advances in ApoA-Ⅰmimic peptides against atherosclerosis

作　　者：贺春霞 李慧瑾 秦魏 邢露 周鑫 赵栋 李鹏权 金曦 曹慧玲 HE Chun-xia;LI Hui-jin;QIN Wei;XING Lu;ZHOU Xin;ZHAO Dong;LI Peng-quan;JIN Xi;CAO Hui-ling(Shaanxi Key Lab of Ischemic Cardiovascular Disease, Institute of Basic and Translational Medicine, Xi’an Medical University, Xi’an 710021, China)

机构地区：[1]陕西省缺血性心血管疾病重点实验室,西安医学院基础与转化医学研究所,陕西西安710021

出　　处：《中国药理学通报》2021年第2期155-160,共6页Chinese Pharmacological Bulletin

基　　金：陕西省教育厅重点科学研究计划项目(No 17JS117)。

摘　　要：载脂蛋白A-I(apolipoprotein A-I,ApoA-Ⅰ)是高密度脂蛋白(high density lipoprotein,HDL)的主要蛋白成分,在胆固醇逆转运(reverse cholesterol transport,RCT)中发挥关键作用,是抗动脉粥样硬化(atherosclerosis,As)药物研发的重要靶标。靶向ApoA-Ⅰα螺旋研发的模拟肽和基于重组ApoA-Ⅰ研发的HDL模拟肽已进入临床试验,展示了良好的促RCT与抗As活性。本文综述了ApoA-Ⅰ的结构和功能,ApoA-Ⅰ与ABCA1(ATP-binding cassette transporter A1)、LCAT(lecithin cholesterol acyl transferase)、SR-B1(scavenger receptor class B type 1)的分子互作机制,总结了靶向ApoA-Ⅰ模拟肽的研究进展,以期为模拟肽类抗As新药研发提供参考。Apolipoprotein A-I(ApoA-Ⅰ),the main protein component of high density lipoprotein(HDL),which plays a key role in the process of reverse cholesterol transport(RCT),is considered as an important anti-atherosclerosis(As)drug target.ApoA-Ⅰmimic peptides developed based on itsα-helix,and HDL mimic peptides that developed by recombinant ApoA-Ⅰhave entered clinical trials,exhibiting favorable RCT promotion and anti-As activity.The paper reviewed the advances in the structure and function of ApoA-Ⅰ,the molecular interaction mechanism between ApoA-Ⅰand ABCA1(ATP-binding cassette transporter A1),LCAT(lecithin cholesterol acyl transferase)and SR-B1(scavenger receptor class B type 1),and anti-As activity of ApoA-Ⅰmimic peptides,which would provide references for anti-As new drug development based on ApoA-Ⅰmimic peptides.

关 键 词：载脂蛋白A-Ⅰ 高密度脂蛋白 胆固醇逆转运 动脉粥样硬化 ApoA-Ⅰ模拟肽 Α螺旋 

分 类 号：R341[医药卫生—基础医学] R341.6