Progress Research of Novel Lipid-lowering Therapy of Proprotein Convertase Subtilisin/ kexin Type 9 Inhibitors
10.3870/j.issn.1004-0781.2018.02.008
- VernacularTitle:新一代降脂药物PCSK9抑制药研究进展
- Author:
Yue CHENG
1
;
Xi WANG
Author Information
1. 武汉大学人民医院心内科
- Keywords:
Proprotein convertase subtilisn/ kexin type 9 inhibitor;
Low density lipoprotein receptor;
Low density lipoprotein cholesterol;
Monoclonal antibody
- From:
Herald of Medicine
2018;37(2):178-182
- CountryChina
- Language:Chinese
-
Abstract:
Proprotein convertase subtilisin/ kexin type 9 (PCSK9) is a newly discovered serine protease belonging to the pro-protein family. After being synthesized and secreted by the liver, PCSK9 can be transported in conjunction with low density lipoprotein receptor (LDLR) on the cell surface into lysosomes for degrading LDLR, so that the plasma level of low density lipoprotein cholesterol (LDL-C) failed to be degraded due to the receptor deficiency, which resulted in a rise in plasma LDL-C.PCSK9 inhibitors can effectively inhibit the function of PCSK9 to reduce the level of blood lipids suggested a therapeutic target for the treatment of hypercholesterolemia, which can not only reduce the incidence of cardiovascular events together with the adverse reactions, but also can reverse the development of atherosclerosis and coronary heart disease.This review mainly states that the discovery of PCSK9 targets, the function of PCSK9, and the current status of major PCSK9 inhibitors.
