An electrophoretic mobility shift assay for the identification and kinetic analysis of acetyl transferase inhibitors

被引：12

作者：

Fanslau, Caroline ^{[1
]}

Pedicord, Donna ^{[1
]}

Nagulapalli, Sujatha ^{[2
]}

Gray, Hillary ^{[2
]}

Pang, Suhong ^{[2
]}

Jayaraman, Lata ^{[2
]}

Lippy, Jonathan ^{[3
]}

Blat, Yuval ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Mechanist Biochem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Discovery Biol, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Co, Lead Evaluat, Princeton, NJ 08543 USA

来源：

ANALYTICAL BIOCHEMISTRY | 2010年 / 402卷 / 01期

关键词：

Electrophoretic mobility shift assay; Acetyl transferase; GCN5; GCN5 TRANSCRIPTIONAL COACTIVATOR; HISTONE ACETYLTRANSFERASE GCN5; P300/CBP-ASSOCIATED FACTOR; CATALYTIC MECHANISM; SUBSTRATE; P300; HATS; PCAF;

D O I：

10.1016/j.ab.2010.03.025

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Histone acetyl transferases are important regulators of cellular homeostasis. This study describes a sensitive acetyl transferase electrophoretic mobility shift assay applicable both for kinetic analysis of acetyl transferase inhibitors and for high-throughput testing. Application of the assay for human GCN5L2 enabled dissection of inhibitor competition with respect to acetyl coenzyme A. Furthermore, we demonstrated that the assay can detect time-dependent inhibition of human GCN5L2 by reactive inhibitors. (C) 2010 Elsevier Inc. All rights reserved.

引用

页码：65 / 68

页数：4

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