Journal article
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability
- Abstract:
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Ligands for the bromodomain and extra-terminal domain (BET) family of bromodomains have shown promise as useful therapeutic agents for treating a range of cancers and inflammation. Here we report that our previously developed 3,5-dimethylisoxazole-based BET bromodomain ligand (OXFBD02) inhibits interactions of BRD4(1) with the RelA subunit of NF-κB, in addition to histone H4. This ligand shows a promising profile in a screen of the NCI-60 panel but was rapidly metabolised (t½ = 39.8 min). Str...
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- Publication status:
- Published
- Peer review status:
- Peer reviewed
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(Version of record, pdf, 3.3MB)
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- Publisher copy:
- 10.1016/j.bmc.2018.05.003
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Authors
Funding
German Research Foundation
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GlaxoSmithKline
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Bibliographic Details
- Publisher:
- Elsevier Publisher's website
- Journal:
- Bioorganic and Medicinal Chemistry Journal website
- Volume:
- 26
- Issue:
- 11
- Pages:
- 2937-2957
- Publication date:
- 2018-05-15
- Acceptance date:
- 2018-05-02
- DOI:
- EISSN:
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1464-3391
- ISSN:
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0968-0896
- Pmid:
-
29776834
- Source identifiers:
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852973
Item Description
- Language:
- English
- Keywords:
- Pubs id:
-
pubs:852973
- UUID:
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uuid:8a90387b-56d0-4a89-89fd-ead0042e89c7
- Local pid:
- pubs:852973
- Deposit date:
- 2018-05-24
Terms of use
- Copyright holder:
- Filippakopoulos et al
- Copyright date:
- 2018
- Notes:
- © 2018 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
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