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PCSK9的药理学筛选靶点 被引量：1

Selecting Pharmacological Targets of PCSK9
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摘要 前蛋白转化酶枯草溶菌素9(PCSK9)基因编码神经凋亡调节转化酶即NARC1,通过影响肝LDLR水平,在胆固醇代谢中发挥了重要的作用.其功能获得型突变使血浆胆固醇水平增高,而功能缺失型突变降低胆固醇水平.流行病学调查显示,高胆固醇血症是动脉粥样硬化和心脏病的主要危险因素.一些患者运用当前的降胆固醇药物治疗仍不能达到推荐的目标LDL水平,PCSK9作为新的降脂靶点引起了广泛的关注.本文将对PCSK9的结构、功能和药理学靶点进行综述. Hypercholesterolemia is a major risk factor for atherosclerosis and heart disease. Current cholesterol-limiting therapies fail in some patients, where additional therapeutic targets are needed. PCSK9 encodes a pro-protein convertase subtitisin/kexin type 9a that plays an important role in cholesterol metabolism by the modulation of LDL receptor levels in the liver. Gain-of-function mutations of PCSK9 resulted in elevated levels of LDL-cholesterol in the plasma. Loss-of-function mutations led to high levels of the LDL receptor and low LDL-cholesterol. This review focuses on the structure, functions and pharmacological targets of PCSK9.
作者 武春艳 唐志晗 刘录山 姜志胜
机构地区 南华大学心血管疾病研究所
出处 《中国生物化学与分子生物学报》 CAS CSCD 北大核心 2009年第11期991-996,共6页 Chinese Journal of Biochemistry and Molecular Biology
基金 国家自然科学基金资助项目(No.30700325) 湖南省应用基础研究计划重点项目(2008FJ2006)资助 湖南省高校科技创新团队支持计划资助~~
关键词 前蛋白转化酶枯草溶菌素9 高胆固醇血症 药理学靶点 pro-protein convertase subtilisin/kexin 9 （PCSKg） hypercholesterinemia pharmacology target
分类号 Q789 [生物学—分子生物学]
  • 相关文献

参考文献20

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二级参考文献44

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共引文献24

同被引文献30

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二级引证文献9

中国生物化学与分子生物学报
2009年 第11期

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