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Structural features and inhibitors of bromodomains
Jamel Meslamani1, Steven G Smith1, Roberto Sanchez1
1Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, 1425 Madison Avenue, New York, NY 10029, United States.
Drug Discovery Today. Technologies
|October 23, 2016
Summary
Bromodomains, crucial for gene regulation, are key targets for treating diseases like cancer. This review covers bromodomain inhibitors, focusing on structural insights to improve drug development for better affinity and selectivity.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Bromodomains are protein modules that bind acetylated lysine residues on histone tails and other proteins.
- These interactions are vital for regulating gene transcription within chromatin.
- BET family bromodomains are particularly important and represent druggable targets for various human diseases.
Purpose of the Study:
- To review the structural and functional characteristics of bromodomains.
- To discuss small-molecule inhibitors targeting bromodomains.
- To provide new insights into bromodomain ligand-binding sites for improved inhibitor design.
Main Methods:
- Literature review of structural and functional studies on bromodomains.
- Analysis of existing small-molecule inhibitors and their mechanisms.
- Examination of ligand-binding site landscapes within bromodomains.
Main Results:
- Bromodomains play a critical role in gene transcription regulation.
- BET family bromodomains are validated targets for therapeutic intervention in cancer and inflammation.
- Small-molecule inhibitors targeting bromodomains have been developed, with ongoing efforts to enhance their affinity and selectivity.
Conclusions:
- Understanding bromodomain structure-function relationships is essential for drug discovery.
- Targeting bromodomains offers a promising therapeutic strategy for various diseases.
- Further research into ligand-binding sites will accelerate the development of more effective bromodomain inhibitors.
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