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Evaluation of linker length effects on a BET bromodomain probe

Abstract:

Fueled by the therapeutic potential of the epigenetic machinery, BET bromodomains have seen high interest as drug targets. Herein, we introduce different linkers to a BET bromodomain benzodiazepine ligand (I-BET762) to gauge its implications in the development of hybrid drugs, imaging probes and small molecule drug conjugates. Biophysical studies confirmed minimal disruption to binding of the BRD4 cavity by the synthesized entities, which includes imaging probes. Target engagement was confirm...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/c9cc05054j

Authors


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Institution:
University of Oxford
Department:
NDM
Sub department:
NDM Experimental Medicine
Role:
Author
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Institution:
University of Oxford
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
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Name:
Medical Research Council
Grant:
MR/N010051/1
Publisher:
Royal Society of Chemistry
Journal:
Chemical Communications More from this journal
Volume:
55
Issue:
68
Pages:
10128-10131
Publication date:
2019-08-01
Acceptance date:
2019-08-01
DOI:
ISSN:
1359-7345 and 1364-548X
Pmid:
31386708
Language:
English
Keywords:
Pubs id:
pubs:1041560
UUID:
uuid:094e185d-dc0c-49e6-9b70-4dc08b2792f3
Local pid:
pubs:1041560
Source identifiers:
1041560
Deposit date:
2020-01-07

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