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Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors.

Abstract:

Small molecule modulators of epigenetic processes are currently sought as basic probes for biochemical mechanisms, and as starting points for development of therapeutic agents. N(epsilon)-Methylation of lysine residues on histone tails is one of a number of post-translational modifications that together enable transcriptional regulation. Histone lysine demethylases antagonize the action of histone methyltransferases in a site- and methylation state-specific manner. N(epsilon)-Methyllysine dem...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1371/journal.pone.0015535

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Institution:
University of Oxford
Role:
Author
More by this author
Institution:
University of Oxford
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
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Institution:
University of Oxford
Role:
Author
Structural Genomics Consortium More from this funder
Biotechnology and Biological Research Council More from this funder
Wellcome Trust More from this funder
National Institutes of Health More from this funder
Commonwealth Scholarship Commission in the United Kingdom More from this funder
Publisher:
Public Library of Science Publisher's website
Journal:
PloS one Journal website
Volume:
5
Issue:
11
Article number:
e15535
Publication date:
2010-01-01
DOI:
EISSN:
1932-6203
ISSN:
1932-6203
Language:
English
Keywords:
UUID:
uuid:c6104d70-028f-46bd-b02d-223982e7f869
Local pid:
pubs:99853
Source identifiers:
99853
Deposit date:
2012-12-19

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