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Assessing histone demethylase inhibitors in cells: lessons learned

Abstract:

Background
Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders. The first KDM inhibitors for KDM1 have entered clinical trials, and efforts are ongoing to develop potent, selective and cell-active ‘probe’ molecules for this target class. Robust cellular assays to assess the specific engagement of KDM inhibitors in cells as well as their c...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1186/s13072-017-0116-6

Authors


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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
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More from this funder
Grant:
FP7/2007-2013) Innovative Medicines Initiative Joint Undertaking under Grant Agreement No. 115766
European Federation of Pharmaceutical Industries and Associations More from this funder
Publisher:
BioMed Central Publisher's website
Journal:
Epigenetics and Chromatin Journal website
Volume:
10
Issue:
9
Publication date:
2017-03-01
Acceptance date:
2017-02-21
DOI:
EISSN:
1756-8935
ISSN:
1756-8935
Source identifiers:
684169
Keywords:
Pubs id:
pubs:684169
UUID:
uuid:5c854f9a-6888-478c-85f9-b4a155f8b999
Local pid:
pubs:684169
Deposit date:
2017-03-07

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