Design, synthesis and characterization of covalent KDM5 inhibitors

Histone lysine demethylases (KDMs) are involved in the dynamic regulation of gene expression and they play a critical role in several biological processes. Achieving selectivity over the different KDMs has been a major challenge for KDM inhibitor development. Here we report potent and selective KDM5...

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Bibliographic Details
Main Authors:	Vazquez-Rodriguez, S, Wright, M, Rogers, C, Cribbs, A, Velupillai, S, Philpott, M, Lee, H, Dunford, J, Huber, K, Robers, M, Vasta, J, Thezenas, M, Bonham, S, Kessler, B, Bennett, J, Fedorov, O, Raynaud, F, Donovan, A, Blagg, J, Bavetsias, V, Oppermann, U, Bountra, C, Kawamura, A, Brennan, P
Format:	Journal article
Language:	English
Published:	John Wiley and Sons, Ltd. 2018

Design, synthesis and characterization of covalent KDM5 inhibitors

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