Potent and selective KDM5 inhibitor stops cellular demethylation of H3K4me3 at transcription start sites and proliferation of MM1S myeloma cells

<p>Methylation of lysine residues on histone tail is a dynamic epigenetic modification that plays a key role in chromatin structure and gene regulation. Members of the KDM5 (also known as JARID1) sub-family are 2-oxoglutarate (2-OG) and Fe2+-dependent oxygenases acting as histone 3 lysine 4 tr...

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Bibliographic Details
Main Authors: Tumber, A, Nuzzi, A, Hookway, E, Hatch, S, Velupillai, S, Johansson, C, Kawamura, A, Savitsky, P, Yapp, C, Szykowska, A, Wu, N, Bountra, C, Strain-Damerell, C, Burgess-Brown, N, Ruda, G, Fedorov, O, Munro, S, England, K, Nowak, R, Schofield, C, La Thangue, N, Pawlyn, C, Davies, F, Morgan, G, Athanasou, N, Müller, S, Oppermann, U, Brennan, P
Format: Journal article
Language:English
Published: Elsevier 2017