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Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2

Abstract:

The polyadenosine-diphosphate-ribose polymerase 14 (PARP14) has been implicated in DNA damage response pathways for homologous recombination. PARP14 contains three (ADP ribose binding) macrodomains (MD) whose exact contribution to overall PARP14 function in pathology remains unclear. A medium throughput screen led to the identification of N-(2(-9H-carbazol-1-yl)phenyl)acetamide (GeA-69, 1) as a novel allosteric PARP14 MD2 (second MD of PARP14) inhibitor. We herein report medicinal chemistry a...

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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.bmc.2018.03.020

Authors


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Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Role:
Author
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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM; Structural Genomics Consortium
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM; Structural Genomics Consortium
Role:
Author
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Structural Genomics Consortium More from this funder
Publisher:
Elsevier Publisher's website
Journal:
Bioorganic and Medicinal Chemistry Journal website
Volume:
26
Issue:
11
Pages:
2965-2972
Publication date:
2018-03-12
Acceptance date:
2018-03-10
DOI:
EISSN:
1464-3391
ISSN:
0968-0896
Pubs id:
pubs:829044
URN:
uri:edf58132-1261-4d58-8102-7783253d1470
UUID:
uuid:edf58132-1261-4d58-8102-7783253d1470
Local pid:
pubs:829044

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