- Abstract:
-
Bromodomain‐containing proteins are epigenetic modulators involved in a wide range of cellular processes, from recruitment of transcription factors to pathological disruption of gene regulation and cancer development. Since the druggability of these acetyl‐lysine reader domains was established, efforts were made to develop potent and selective inhibitors across the entire family. Here we report the development of a small molecule‐based approach to covalently modify recombinant and endogenous ...
Expand abstract - Publication status:
- Published
- Peer review status:
- Peer reviewed
- Version:
- Publisher's version
- Files:
-
-
(pdf, 3.2mb)
-
(pdf, 3.5mb)
-
- Publisher copy:
- 10.1002/anie.201807825
-
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- Publisher:
- Wiley Publisher's website
- Journal:
- Angewandte Chemie International Edition Journal website
- Volume:
- 58
- Issue:
- 4
- Pages:
- 1007-1012
- Publication date:
- 2018-12-27
- Acceptance date:
- 2018-12-27
- DOI:
- EISSN:
-
1521-3773
- ISSN:
-
1433-7851
- Pubs id:
-
pubs:954996
- URN:
-
uri:39db9ad9-8705-4423-8ca6-f035504f2873
- UUID:
-
uuid:39db9ad9-8705-4423-8ca6-f035504f2873
- Local pid:
- pubs:954996
- Language:
- English
- Keywords:
- Copyright holder:
- D'Ascenzio et al.
- Copyright date:
- 2018
- Notes:
-
Copyright © 2019 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.
This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
Journal article
An activity-based probe targeting non-catalytic, highly conserved amino acid residues within bromodomains
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