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Bromodomain Histone Readers and Cancer
Abhinav K Jain1, Michelle C Barton2
1Department of Epigenetics & Molecular Carcinogenesis, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA; Center for Stem Cell & Development Biology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA; Center for Cancer Epigenetics, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.
Journal of Molecular Biology
|November 29, 2016
Summary
Histone lysine acetylation regulates gene transcription and chromatin structure. Bromodomain inhibitors targeting these epigenetic readers show promise for cancer drug discovery.
Area of Science:
- Epigenetics
- Molecular Biology
- Cancer Biology
Background:
- Lysine acetylation of histone proteins is a key post-translational modification regulating gene transcription and chromatin structure.
- Aberrant histone acetylation is linked to various diseases, particularly cancers.
- Acetyl-lysine modifications serve as binding sites for bromodomain-containing 'reader' proteins involved in transcription regulation.
Purpose of the Study:
- To review bromodomain-containing proteins with established roles in cancer.
- To highlight recent advancements in the development of bromodomain inhibitors for therapeutic applications.
Main Methods:
- Literature review focusing on bromodomain proteins in cancer.
- Analysis of recent progress in medicinal chemistry for bromodomain inhibitor development.
Main Results:
- Bromodomain-containing proteins are frequently dysregulated in cancers, influencing oncogene and anti-apoptotic protein expression.
- Development of structurally guided chemical probes targeting bromodomains is advancing.
Conclusions:
- Bromodomain readers of histone acetylation represent promising therapeutic targets for cancer treatment.
- Epigenetic-focused drug discovery is crucial for developing novel bromodomain inhibitors.
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