PCSK9抑制剂调脂作用的研究进展  

Research progress on lipid-lowering effects of PCSK9 inhibitors

作　　者：孙丰翠 张世昭 马超群 杨秀芬 鲁海菲 于露 张风霞[3] SUN Feng-cui;ZHANG Shi-zhao;MA Chao-qun;YANG Xiu-fen;LU Hai-fei;YU Lu;ZHANG Feng-xia(The First Clinical Medical College,Shandong University of Traditional Chinese Medicine,Ji-nan SHANDONG 250355,China;School of Traditional Chinese Medicine,Shandong University of Traditional Chinese Medicine,Ji-nan SHANDONG 250355,China;Neurosurgery Department,Affiliated Hospital of Shandong University of Traditional Chinese Medicine,Ji-nan SHANDONG 250011,China)

机构地区：[1]山东中医药大学第一临床医学院,山东济南250355 [2]山东中医药大学中医学院,山东济南250355 [3]山东中医药大学附属医院脑病科,山东济南250011

出　　处：《中国新药与临床杂志》2021年第6期401-406,共6页Chinese Journal of New Drugs and Clinical Remedies

基　　金：国家自然科学基金(81573945);国家中医药管理局王新陆全国名中医工作室项目(鲁财社指[2016]47号);山东省科技计划项目(2013GSF11902);山东省中医药科技发展项目(2013-081、2019-093)。

摘　　要：前蛋白转化酶枯草杆菌蛋白酶9型(PCSK9)与血脂代谢关系密切,其通过竞争性结合低密度脂蛋白受体(LDLR),导致低密度脂蛋白(LDL)降解减少,引发以低密度脂蛋白胆固醇(LDL-C)水平升高为特点的脂代谢紊乱。PCSK9抑制剂可通过抑制PCSK9与LDLR结合、抑制PCSK9表达发挥调脂作用,降低LDL-C水平。目前PCSK9抑制剂主要包括PCSK9单克隆抗体、类抗体蛋白药、模拟肽、小干扰RNA、反义寡核苷酸,以及小分子抑制剂、天然化合物等,其他抑制PCSK9的方法有基因编辑、免疫接种等。Proprotein convertase 9(PCSK9)is closely related to lipid metabolism.It competitively binds to lowdensity lipoprotein receptor(LDLR),resulting in reduced degradation of low-density lipoprotein(LDL),and leading to lipid metabolism disorder characterized by increased level of low-density lipoprotein cholesterol(LDL-C).PCSK9 inhibitors can reduce LDL-C level by inhibiting the binding of PCSK9 to LDLR and the expression of PCSK9.At present,PCSK9 inhibitors mainly include PCSK9 monoclonal antibodies,antibody-like protein drugs,mimetic peptides,small interfering RNA,antisense oligonucleotides,small molecule inhibitors,and natural compounds.Other methods to inhibit PCSK9 include gene editing,immunizations,etc.

关 键 词：前蛋白转化酶9 胆固醇 LDL 受体 LDL 高胆固醇血症 

分 类 号：R541.4[医药卫生—心血管疾病] R972.6[医药卫生—内科学]