一种香豆素荧光标记多肽的合成及应用

doi:10.3724/SP.J.1095.2014.40090

摘要/Abstract

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

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.

Key words: histone deacetylase, Sirtuin, SIRT5, fluorescently labeled peptides

中图分类号:

O654

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, DOI: 10.3724/SP.J.1095.2014.40090.

LI Yan1, LIU Xiaoyan2,4, ZHANG Shun2,4, LIU Ting3,4, LI Yongjun2,4, LAN Yanyu2,4, WANG Aimin2,4, WANG Yonglin3,4, HE Bin3,4*. Synthesis and Application of a Coumarin Fluorescently Labeled Peptide[J]. Chinese Journal of Applied Chemistry, DOI: 10.3724/SP.J.1095.2014.40090.

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