Design, synthesis and characterization of covalent KDM5 inhibitors

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

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