The DOI matches its Crossref record; 16 of the 16 references it cites were found in a registry or an index.
Bromodomains as therapeutic targets
Open accessAbstract
Acetylation of lysine residues is a post-translational modification with broad relevance to cellular signalling and disease biology. Enzymes that ‘write’ (histone acetyltransferases, HATs) and ‘erase’ (histone deacetylases, HDACs) acetylation sites are an area of extensive research in current drug development, but very few potent inhibitors that modulate the ‘reading process’ mediated by acetyl lysines have been described. The principal readers of ɛ-N-acetyl lysine (Kac) marks are bromodomains (BRDs), which are a diverse family of evolutionary conserved protein-interaction modules. The conserved BRD fold contains a deep, largely hydrophobic acetyl lysine binding site, which represents an attractive pocket for the development of small, pharmaceutically active molecules. Proteins that contain BRDs have been implicated in the development of a large variety of diseases. Recently, two highly potent and selective inhibitors that target BRDs of the BET (bromodomains and extra-terminal) family provided compelling data supporting targeting of these BRDs in inflammation and in an aggressive type of squamous cell carcinoma. It is likely that BRDs will emerge alongside HATs and HDACs as interesting targets for drug development for the large number of diseases that are caused by aberrant acetylation of lysine residues.
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Cites
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Cited by
Accurate calculation of the absolute free energy of binding for drug molecules
Aldeghi, M., Heifetz, A., Bodkin, M. J., Knapp, S., & Biggin, P. C. (2016) · Chemical Science · doi:10.1039/c5sc02678d · Cited by 347
Self-citationInhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma
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Self-citationBromodomain‐dependent stage‐specific male genome programming by Brdt
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Crowe, B. L., Larue, R. C., Yuan, C., Hess, S., Kvaratskhelia, M., & Foster, M. P. (2016) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1516813113 · Cited by 83
Metadata
- Authors
- Muller, S., Filippakopoulos, P., & Knapp, S.
- Venue
- Expert Reviews in Molecular Medicine
- Publisher
- Cambridge University Press (CUP)
- Published
- 2011-09
- Volume
- 13
- Pages
- e29-e29
- ISSN
- 1462-3994 (ISSN-L)
- OpenAlex
- W2114763268
- Cited by
- 442
- References
- 16
- FWCI
- 9.87
- Type
- journal article
- Language
- en
- Open access
- bronze
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