A FRET-based assay for screening SIRT6 modulators
A FRET-based assay for screening SIRT6 modulators
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基于 FRET 的 SIRT6 调节剂筛选分析
DOI：
10.1016/j.ejmech.2015.04.008
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发表时间：
2015-05-26
影响因子：
6.7
通讯作者：
He, Bin
中科院分区：
文献类型：
--
作者：
Li, Yan;You, Ling;He, Bin
SIRT6作为这7种sirtuins中的一种，已被证明具有治疗多种人类疾病的潜力。基于最近发现SIRT6是一种脂肪酰化酶（去除长链脂肪酰基），已经开发了SIRT6的荧光测定来筛选它们的小分子调节剂。然而，该试验使用含有7-氨基-4-甲基香豆素（AMC）的荧光肽，这成为筛选中假阳性的原因。为了克服这个问题，我们开发了一种替代方法，称为基于fret的检测方法，适用于筛选SIRT6调节剂，该方法在高通量格式下可靠且有用，因为该检测中不存在AMC组。(C) 2015 Elsevier Masson SAS。版权所有。
SIRT6, as one of these seven sirtuins, has been shown to have the therapeutic potentials for treating several human diseases. A fluorogenic assay for SIRT6 has been developed to screen their small molecule modulators based on the recent discovery that SIRT6 is a defatty-acylase (removing long chain fatty acyl groups). However, this assay uses a fluorogenic peptide containing 7-amino-4-methylcoumarin (AMC), which becomes the cause of false positive hits from screenings. To overcome this, we have developed an alternative method called a FRET-based assay suitable for screening SIRT6 modulators, which will be reliable and useful in a high-throughput format since no AMC group present in this assay. (C) 2015 Elsevier Masson SAS. All rights reserved.