- Abstract:
-
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...
Expand abstract - Publication status:
- Published
- Peer review status:
- Peer reviewed
- Version:
- Publisher's version
- Files:
-
-
(pdf, 3.3MB)
-
- Publisher copy:
- 10.1016/j.bmc.2018.05.003
-
Version unsuitable
-
We have not obtained a suitable full-text for a given research output. See this page for more information.
-
Recently completed
-
Sometimes content is held in ORA but is unavailable for a fixed period of time to comply with the policies and wishes of rights holders.
-
Permissions
-
All content made available in ORA should comply with relevant rights, such as copyright. See this page for more information.
-
Clearance
-
Some thesis volumes scanned as part of the digitisation scheme funded by Dr Leonard Polonsky are currently unavailable due to sensitive material or uncleared third-party copyright content. We are attempting to contact authors whose theses are affected.
- 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:
-
1464-3391
- ISSN:
-
0968-0896
- Pubs id:
-
pubs:852973
- URN:
-
uri:8a90387b-56d0-4a89-89fd-ead0042e89c7
- UUID:
-
uuid:8a90387b-56d0-4a89-89fd-ead0042e89c7
- Local pid:
- pubs:852973
- Language:
- English
- Keywords:
- 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/).
Journal article
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability
Actions
Access Document
Why is the content I wish to access not available via ORA?
Bibliographic data (the information relating to research outputs) and full-text items (e.g. articles, theses, reports, etc.) arrive in ORA from several different sources. Unfortunately we are not able to make available the full-text for every research output.
Please contact the ORA team (
) if you have queries regarding unavailable content OR if you are aware of a full-text copy we can make available.
) if you have queries regarding unavailable content OR if you are aware of a full-text copy we can make available.
Content may be unavailable for the following four reasons
Alternative access to the full-text
You may be able to access the full-text directly from the publisher's website using the 'Publisher Copy' link in the 'Links & Downloads' box from a research output's ORA record page. This method may require an institutional or individual subscription to the journal/resource.
Authors
Funding
GlaxoSmithKline
More from this funder
German Research Foundation
More from this funder
Expand funders...
Bibliographic Details
Item Description
Terms of use
If you are the owner of this record, you can report an update to it here: Report update to this record