期刊论文

Tang, Zhi-Han;Liu, Lu-Shan

英文

中国药理学报

1671-4083

2017

38

3

301-311

10.1038/aps.2016.134

National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81200217, 81370376]; Natural Science Foundation of Hunan provinceNatural Science Foundation of Hunan Province [2015JJ4097]; Key Project of Science and Technology Department of Hunan Province [2015JC3081]; Key Project of the Educational Department of Hu-nan Province [15A137]; Visiting Scholar Foundation of Key Laboratory of Biorheological Science and Technology (Chongqing University); Ministry of Education [CQKLBST-2014-002, CQKLBST-2015-004]; Construct Program of the Key Discipline in Hunan Province

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Proprotein convertase subtilisin/kexin type 9 (PCSK9), also known as neural apoptosis regulated convertase (NARC1), is a key modulator of cholesterol metabolism. PCSK9 increases the serum concentration of low-density lipoprotein cholesterol by escorting low-density lipoprotein receptors (LDLRs) from the membrane of hepatic cells into lysosomes, where the LDLRs are degraded. Owing to the importance of PCSK9 in lipid metabolism, considerable effort has been made over the past decade in developing drugs targeting PCSK9 to lower serum lipid levels. Nevertheless, some problems and challenges remain...

Proprotein convertase subtilisin/kexin 类型 9 (PCSK9 ) ，也已知的同样神经的 apoptosis 调整了 convertase (NARC1 ) ，是胆固醇新陈代谢的一个关键调节的人。PCSK9 由从肝的房间的膜陪同低密度的脂蛋白受体(LDLR ) 进 lysosomes 增加低密度的脂蛋白胆固醇的浆液集中，在 LDLR 被降级的地方。由于在类脂化合物新陈代谢的 PCSK9 的重要性，可观的努力在开发指向 PCSK9 降低浆液类脂化合物层次的药在过去的十年被作了。不过，一些问题和挑战留下。在这评论我们首先描述 PCSK9 和它的基因多型性的结构和功能。我们然后讨论 PCSK9 的药理学目标的各种各样的图案，包括堵住到肝的 LDLR (模仿的肽...