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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

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Publisher copy:
10.1016/j.chembiol.2017.02.006

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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
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Institution:
University of Oxford
Division:
MSD
Department:
NDORMS
Role:
Author
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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Role:
Author
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Funding agency for:
Kawamura, A
Grant:
Dorothy Hodgkin Research Fellow
Novartis Pharma AG 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
Language:
English
Keywords:
Pubs id:
pubs:684148
UUID:
uuid:ed7f02af-e1f0-49ca-b094-477e2a4b81fb
Local pid:
pubs:684148
Deposit date:
2017-03-07

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