| 陈曦 刘伯宁 杨赟 陈启 王皓.PCSK9 单克隆抗体作用机制与临床研究进展[J].,2016,16(6):1156-1160 |
| PCSK9 单克隆抗体作用机制与临床研究进展 |
| Clinical Research of Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9)Monoclonal Antibodies |
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| DOI： |
| 中文关键词: 前蛋白转化酶枯草溶菌素9 低密度脂蛋白受体 低密度脂蛋白胆固醇 高胆固醇血症 单克隆抗体 |
| 英文关键词: PCSK9 Low density lipoprotein (LDL) Low density lipoprotein receptor(LDLR) Hypercholesterolemia Monoclonal
antibody（mAb） |
| 基金项目:国家自然科学基金项目（81330061）；科技部973 计划项目（2010CB833605）；国家863 计划项目（2014AA021004） |
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| 中文摘要: |
| 前蛋白转化酶枯草溶菌素9（PCSK9）是前蛋白转化酶家族成员之一，它通过与肝细胞表面低密度脂蛋白受体（LDLR)结合，
使体内低密度脂蛋白水平升高，引发高血脂。PSCK9抑制剂可以达到降低血脂的临床效果并已经成为重要的减少冠心病发病率
的药物靶点。尤其是单克隆抗体药物，作为目前唯一的具有降脂功能的单克隆抗体，在临床试验上的表现对于家族遗传性高血脂
的治疗及冠心病的防治都具有重要意义。本文将主要对PCSK9 的作用机制及其单克隆抗体的研发现状、临床试验进展进行总结，
旨在对降脂单抗药物研发与临床应用作为参考。 |
| 英文摘要: |
| Proprotein convertase subtilisin kexin type 9 (PCSK9) is a member of subtilisin-like proprotein convertase family. By
interacting with low density lipoprotein receptor (LDLR) on the surface of hepatocyte, PCSK9 plays an important role in elevating the
level of low density lipoprotein (LDL) and finally leading to hyperlipidemia. The PCSK9-inhibitor is now being an important and totally
new therapeutic target to reduce the incidence of coronary heart disease through its function of lipid lowering. Especially, as the only
theraputic antibody-drug with lipid-lowering function, the lipid depressing effect of monoclonal antibodies has crucial meaning for the
therapy of familial transmissibility hyperlipidemia and the prevention of coronary heart disease. In this article, the mechanism of PCSK9,
the research and development status, the safety and clinical efficacy of PCSK9 monoclonal antibodies will be briefly reviewed, with the
purpose to provide important reference for research and development of monoclonal antibodies to PCSK9. |
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