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Pubmed ID :28262558
Publication Date : //

Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.


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 Fe-dependent oxygenases acting as histone 3 lysine 4 trimethyl (H3K4me3) demethylases, regulating proliferation, stem cell self-renewal, and differentiation. Here we present the characterization of KDOAM-25, an inhibitor of KDM5 enzymes. KDOAM-25 shows biochemical half maximal inhibitory concentration values of <100 nM for KDM5A-D in vitro, high selectivity toward other 2-OG oxygenases sub-families, and no off-target activity on a panel of 55 receptors and enzymes. In human cell assay systems, KDOAM-25 has a half maximal effective concentration of ∼50 μM and good selectivity toward other demethylases. KDM5B is overexpressed in multiple myeloma and negatively correlated with the overall survival. Multiple myeloma MM1S cells treated with KDOAM-25 show increased global H3K4 methylation at transcriptional start sites and impaired proliferation.

Authors : Tumber Anthony , Nuzzi Andrea , Hookway Edward S , Hatch Stephanie B , Velupillai Srikannathasan , Johansson Catrine , Kawamura Akane , Savitsky Pavel , Yapp Clarence , Szykowska Aleksandra , Wu Na , Bountra Chas , Strain-Damerell Claire , Burgess-Brown Nicola A , Ruda Gian Filippo , Fedorov Oleg , Munro Shonagh , England Katherine S , Nowak Radoslaw P , Schofield Christopher J , La Thangue Nicholas B , Pawlyn Charlotte , Davies Faith , Morgan Gareth , Athanasou Nick , Müller Susanne , Oppermann Udo , Brennan Paul E ,

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