综述

PCSK9 抑制剂降低低密度脂蛋白胆固醇的临床研究进展

  • 季海英 ,
  • 尤纱纱 ,
  • 曹惠敏 ,
  • 何斌
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  • 上海交通大学 医学院附属新华医院麻醉与重症医学科,上海 200092
季海英(1992—),女,硕士生;电子信箱:h_ying716@163.com。

网络出版日期: 2018-03-09

基金资助

 国家自然科学基金(81470390);上海市教育委员会高峰高原学科建设计划(20152218);上海申康临床三年行动计划项目(16CR3006A);上海市科
学技术委员会科研计划项目(17411954700)

Clinical research of PCSK9 inhibitors in reducing low density lipoprotein cholesterol

  • JI Hai-ying ,
  • YOU Sha-sha ,
  • CAO Hui-min ,
  • HE Bin
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  • Department of Anesthesiology and SICU, Xinhua Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China

Online published: 2018-03-09

Supported by

National Natural Science Foundation of China, 81470390; Shanghai Municipal Education Commission—Gaofeng Clinical
Medicine Grant Support, 20152218; Clinical Research Plan of Shanghai Hospital Development Center, 16CR3006A; Program of Science and Technology Commission of Shanghai Municipality, 17411954700

摘要

[ 摘要 ] 低密度脂蛋白胆固醇 ( LDL-C) 水平升高是心血管疾病的主要危险因素。前蛋白转换酶枯草溶菌素 9(proprotein convertase
subtilisin/kexin type 9,PCSK9)来源于肝细胞,能降解低密度脂蛋白受体,导致肝摄取的胆固醇减少、循环中的 LDL-C 增多。PCSK9
抑制剂能够使肝细胞表面的低密度脂蛋白受体的水平升高,进而结合更多的 LDL-C,从而降低血 LDL-C 的水平。因此,PCSK9 成为
防治心血管疾病、开发新型降脂药物的热门靶点。现主要对 PCSK9 的作用机制及其抑制剂的研发历史、作用机制、体内代谢过程以
及主要临床试验结果进行总结。

本文引用格式

季海英 , 尤纱纱 , 曹惠敏 , 何斌 . PCSK9 抑制剂降低低密度脂蛋白胆固醇的临床研究进展[J]. 上海交通大学学报(医学版), 2018 , 38(2) : 212 . DOI: 10.3969/j.issn.1674-8115.2018.02.018

Abstract

Elevated low density lipoprotein cholesterol (LDL-C) is a major risk factor for cardiovascular disease. Studies show that proprotein convertase subtilisin/kexin type 9 (PCSK9) is a circulation enzyme and serves a pivotal function in the degradation of low density lipoprotein receptor, which contributes to the decrease in hepatic cholesterol uptake and increase in circulating LDL-C. PCSK9 inhibitor can significantly elevate the surface of low density lipoprotein receptor of liver cells and bond more LDL-C to decrease the level of LDL-C. Thus PCSK9 has emerged as a popular target for the development of new cholesterol lowering drugs and therapeutic intervention of cardiovascular disease. In this article, the history, mechanism of action, metabolic effects of PCSK9 and the clinical outcomes of PCSK9 inhibitors will be briefly reviewed.
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