A FRET-based assay for screening SIRT5 specific modulators

A FRET-based assay for screening SIRT5 specific modulators
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基于 FRET 的 SIRT5 特异性调节剂筛选分析

DOI:
10.1016/j.bmcl.2015.03.018
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发表时间:
2015-04-15
影响因子:
2.7
通讯作者:
He, Bin
He, Bin
中科院分区:
医学4区
文献类型:
--
作者:
Li, Yan;Huang, Wenfei;He, Bin

文献摘要

被引文献

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基于最近发现SIRT 5是一种脱丙二酸酶和脱琥珀酰酶,已经开发了SIRT 5的荧光测定以筛选它们的小分子调节剂。然而,该测定使用含有7-氨基-4-甲基香豆素(AMC)的荧光肽,这成为筛选中假阳性命中的原因。为了克服这一点,我们开发了一种称为基于FRET的测定的替代方法,该方法对于以高通量形式筛选SIRT 5调节剂是可靠和有用的,因为该测定中不存在AMC基团。(C)2015爱思唯尔有限公司版权所有。
A fluorogenic assay for SIRT5 has been developed to screen their small molecule modulators based on the recent discovery that SIRT5 is a demalonylase and desuccinylase. However, this assay uses a fluorogenic peptide containing 7-amino-4-methylcoumarin (AMC), which becomes the cause of false positive hits from the screening. To overcome this, we have developed an alternative method called a FRET-based assay, which will be reliable and useful for screening SIRT5 modulators in a high-throughput format since no AMC group present in this assay. (C) 2015 Elsevier Ltd. All rights reserved.