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

Abstract:

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 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 bioch...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1016/j.chembiol.2017.02.006

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Department:
Oxford, MPLS, Chemistry, Organic Chemistry
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Author
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Department:
Oxford, MSD, NDORMS
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Author
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Department:
Oxford, MSD, NDM, Target Discovery Institute
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Department:
Oxford, MSD, NDM, Structural Genetics Consortium
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Funding agency for:
Kawamura, A
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Funding agency for:
Schofield, CJ
Bayer Pharma AG More from this funder
Boehringer Ingelheim More from this funder
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Publisher:
Elsevier Publisher's website
Journal:
Cell Chemical Biology Journal website
Publication date:
2017-03-02
Acceptance date:
2017-02-01
DOI:
ISSN:
2451-9456
Pubs id:
pubs:684148
URN:
uri:ed7f02af-e1f0-49ca-b094-477e2a4b81fb
UUID:
uuid:ed7f02af-e1f0-49ca-b094-477e2a4b81fb
Local pid:
pubs:684148

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