A chemical toolbox for the study of bromodomains and epigenetic signaling

Bromodomains are conserved protein interaction modules that recognize acetyl-lysine modifications. Here the authors present a set of 25 selective small molecule inhibitors covering 29 human bromodomain targets and comprehensively evaluate the selectivity of this probe-set.

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Detalles Bibliográficos
Autores principales: Qin Wu, David Heidenreich, Stanley Zhou, Suzanne Ackloo, Andreas Krämer, Kiran Nakka, Evelyne Lima-Fernandes, Genevieve Deblois, Shili Duan, Ravi N. Vellanki, Fengling Li, Masoud Vedadi, Jeffrey Dilworth, Mathieu Lupien, Paul E. Brennan, Cheryl H. Arrowsmith, Susanne Müller, Oleg Fedorov, Panagis Filippakopoulos, Stefan Knapp
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2019
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Acceso en línea:https://doaj.org/article/6396da47b45340898d36418988b2a14e
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Descripción
Sumario:Bromodomains are conserved protein interaction modules that recognize acetyl-lysine modifications. Here the authors present a set of 25 selective small molecule inhibitors covering 29 human bromodomain targets and comprehensively evaluate the selectivity of this probe-set.