靶向前蛋白转化酶枯草溶菌素9型（PCSK9）的降脂干预措施：降脂治疗的新篇章。
Lipid-lowering interventions targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): an emerging chapter in lipid-lowering therapy.
作者信息
Kosmas Constantine E, DeJesus Eddy, Morcelo Rosmery, Garcia Frank, Montan Peter D, Guzman Eliscer
机构信息
Department of Medicine, Division of Cardiology, Mount Sinai Hospital, New York, NY, USA.
Department of Medicine, Bronx-Lebanon Hospital Center, Bronx, NY, USA.
出版信息
Drugs Context. 2017 Nov 22;6:212511. doi: 10.7573/dic.212511. eCollection 2017.
Abstract
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease that is mainly expressed in the liver but can also be found in the intestine and kidneys. PCSK9 promotes the degradation of low density lipoprotein receptors (LDLR) by reducing their recycling and targeting the receptors for lysosomal destruction, thereby decreasing the rate of removal of LDL-cholesterol from the circulation. Thus, interventions targeting PCSK9 by reducing its expression may lead to significant reductions of LDL-cholesterol and possibly decrease cardiovascular risk. The present review aims to present and discuss the current clinical and scientific data pertaining to lipid-lowering interventions targeting PCSK9.
摘要
前蛋白转化酶枯草溶菌素/克新9型（PCSK9）是一种丝氨酸蛋白酶，主要在肝脏中表达，但在肠道和肾脏中也可发现。PCSK9通过减少低密度脂蛋白受体（LDLR）的再循环并将这些受体靶向溶酶体进行破坏，从而促进其降解，进而降低LDL胆固醇从循环中清除的速率。因此，通过降低PCSK9的表达来靶向PCSK9的干预措施可能会导致LDL胆固醇显著降低，并有可能降低心血管风险。本综述旨在介绍和讨论与靶向PCSK9的降脂干预措施相关的当前临床和科学数据。
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