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一种香豆素荧光标记多肽的合成及应用
引用本文:李燕,刘晓艳,张顺,刘亭,李勇军,兰燕宇,王爱民,王永林,何彬.一种香豆素荧光标记多肽的合成及应用[J].应用化学,2014,31(12):1413-1418.
作者姓名:李燕  刘晓艳  张顺  刘亭  李勇军  兰燕宇  王爱民  王永林  何彬
作者单位:(贵阳医学院1.基础医学院;2.民族药与中药开发应用教育部工程研究中心; 3.贵州省药物制剂重点实验室;4.药学院 贵阳 550004)
基金项目:国家自然科学基金资助项目(21302027);贵州省中药现代化科技产业研究开发专项项目(黔科合重G字[2013]4001);贵州省科技支撑计划社会发展攻关([2012]3079);贵阳医学院院基金博士启动基金([2014]第015号)~~
摘    要:Sirtuin蛋白是一类称为依赖烟酰胺腺嘌呤二核苷酸(NAD)的组蛋白去乙酰化酶,共有7个成员,均是潜在的疾病治疗靶点。 然而,目前的荧光筛选方法,只适用于SIRT1~SIRT3。 因此,根据SIRT5的新酶活,设计、合成了针对SIRT5的荧光标记多肽(ISGASE(SuK) AMC),并通过LC-MS和荧光检测证明了该荧光标记多肽能应用于SIRT5的活性筛选。

关 键 词:组蛋白去乙酰化酶  Sirtuin  SIRT5  荧光标记多肽  
收稿时间:2014-03-24
修稿时间:2014-06-13

Synthesis and Application of a Coumarin Fluorescently Labeled Peptide
LI Yan;LIU Xiaoyan;ZHANG Shun;LIU Ting;LI Yongjun;LAN Yanyu;WANG Aimin;WANG Yonglin;HE Bin.Synthesis and Application of a Coumarin Fluorescently Labeled Peptide[J].Chinese Journal of Applied Chemistry,2014,31(12):1413-1418.
Authors:LI Yan;LIU Xiaoyan;ZHANG Shun;LIU Ting;LI Yongjun;LAN Yanyu;WANG Aimin;WANG Yonglin;HE Bin
Institution:(1.College of Basic Medical Science; 2.Engineering Research Center for the Development and Application of ; Ethnic Medicine and TCM(Ministry of Education; 3.Guizhou Provincial Key Laboratory of Pharmaceutics,Guiyang Medical College; 4.College of Pharmacy,Guiyang Medical University,Guiyang 550004,China)
Abstract:Sirtuin is a type of nicotinamide adenine dinucleotide(NAD) dependent histone deacetylase, which has seven members. It is a potential therapeutic target for many diseases. However, the present fluorescent screening method is limited to SIRT1~SIRT3. Therefore, based on the discovery of SIRT5′s novel enzymatic activity, we designed and synthesized the fluorescence labeled peptide for SIRT5, ISGASE(SuK)-AMC; and by the validations of LC-MS and fluorescence detection, the fluorescence labeled peptide can be used as a tool to perform the screening based on the enzymatic activity of SIRT5.
Keywords:histone deacetylase  Sirtuin  SIRT5  fluorescently labeled peptides
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