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Discovery of an MLLT1/3 YEATS domain chemical probe

Abstract:

YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug discovery. Dysregulation of these modified lysine binding proteins has been linked to the onset and progression of cancers. We herein report the discovery and characterisation of the first small molecule chemical probe, SGC‐iMLLT, for the YD of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). SGC‐iMLLT is a potent and selective inhibitor of MLLT1/3 ‐ histone interactions. Excellent selectivity over other human...

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

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Publisher copy:
10.1002/anie.201810617

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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Target Discovery Institute
Role:
Author
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John Fell Fund More from this funder
Publisher:
Wiley‐VCH Verlag Publisher's website
Journal:
Angewandte Chemie (International ed. in English) Journal website
Volume:
57
Issue:
50
Pages:
16302-16307
Publication date:
2018-11-16
Acceptance date:
2018-10-05
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
Pubs id:
pubs:925511
URN:
uri:f7a77510-cd4a-40d9-a874-0d755c8a24af
UUID:
uuid:f7a77510-cd4a-40d9-a874-0d755c8a24af
Local pid:
pubs:925511
Language:
English
Keywords:

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