Place your BETs: the therapeutic potential of bromodomains
Abstract
Therapeutic targeting of the processes that regulate histone modification is a growing area of scientific exploration. Although most interest has concentrated on the various families of enzymes that contribute to these processes, this review focuses on emerging data demonstrating the chemical tractability and therapeutic potential of a hitherto underexplored family of proteins, namely the bromodomain (BRD) family of reader proteins. These proteins perform a crucial role in translating histone modifications with powerful transcriptional consequences. We review current knowledge of the biology of this emergent target class and highlight recent breakthroughs that now make the BRD family of reader proteins attractive for drug discovery.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Other bromodomain modules (e.g., BRD4) have proven to be amenable to direct chemical inhibition.
“other bromodomain modules (e.g., BRD4) have proven to be amenable to direct chemical inhibition”
From The transcriptional cofactor TRIM33 prevents apoptosis in B lymphoblastic leukemia by deactivating a single enhancer (2015) · cites this paper as Prinjha et al., 2012
The citation lists haven’t been fetched yet
References 84 · Cited by 197
- Authors
- Prinjha, R. K., Witherington, J., & Lee, K.
- Affiliations
- GlaxoSmithKline (United Kingdom) (GB)
- Corresponding author
- Lee, K.
- ORCID
- Venue
- Trends in Pharmacological Sciences
- Publisher
- Elsevier BV
- Published
- 2012-03
- Volume
- 33
- Issue
- 3
- Pages
- 146-153
- ISSN
- 0165-6147 (ISSN-L)
- OpenAlex
- W2001619812
- Cited by
- 197
- References
- 84
- Citations by year
- 2026: 3 · 2025: 2 · 2024: 4 · 2023: 8 · 2022: 12 · 2021: 13 · 2020: 14 · 2019: 9 · 2018: 9 · 2017: 11 · 2016: 22 · 2015: 32 · 2014: 28 · 2013: 23 · 2012: 7
- FWCI
- 2.71
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Trends in Pharmacological Sciences (publishedVersion)
- PubMed (publishedVersion)
- Funders
- GlaxoSmithKline
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
- Keywords
- bromodomain proteins, histone modifications, histone acetylation, epigenetic drug discovery, BET proteins, transcriptional regulation, small molecule inhibitors
- MeSH terms
- Acetylation, Animals, Histones, Humans, Nuclear Proteins, Gene Expression, Drug Discovery
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
