Journal article
Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit
- Abstract:
-
The acetyl post-translational modification of chromatin at selected histone lysine residues is interpreted by an acetyl-lysine specific interaction with bromodomain reader modules. Here we report the discovery of the potent, acetyl-lysine-competitive, and cell active inhibitor PFI-3 that binds to certain family VIII bromodomains while displaying significant, broader bromodomain family selectivity. The high specificity of PFI-3 for family VIII was achieved through a novel bromodomain binding m...
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- Publication status:
- Published
- Peer review status:
- Peer reviewed
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- Files:
-
-
(Accepted manuscript, pdf, 1.2MB)
-
- Publisher copy:
- 10.1021/acs.jmedchem.6b00012
Authors
Funding
Structural Genomics Consortium
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National Cancer Institute
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Bibliographic Details
- Publisher:
- American Chemical Society Publisher's website
- Journal:
- Journal of Medicinal Chemistry Journal website
- Volume:
- 59
- Issue:
- 10
- Pages:
- 4800-4811
- Publication date:
- 2016-04-26
- Acceptance date:
- 2016-03-01
- DOI:
- EISSN:
-
1520-4804
- ISSN:
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0022-2623
- Pmid:
-
27115555
Item Description
- Language:
- English
- Keywords:
- Pubs id:
-
pubs:619363
- UUID:
-
uuid:0871e410-0fe5-4c79-9579-69030fb2409c
- Local pid:
- pubs:619363
- Source identifiers:
-
619363
- Deposit date:
- 2018-05-22
Terms of use
- Copyright holder:
- American Chemical Society
- Copyright date:
- 2016
- Notes:
- © 2016 American Chemical Society. This is the accepted manuscript version of the article. The final version is available online from American Chemical Society at: https://doi.org/10.1021/acs.jmedchem.6b00012
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