BET Inhibitors as Anticancer Agents: A Patent Review
Imran Ali1, Gildon Choi1, Kwangho Lee1
1Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.
Background:
Bromodomain and Extra Terminal (BET) family of bromodomain proteins (BRDs), comprised of four members in humans (BRD2, BRD3, BRD4, and BRDT), has emerged as a promising new cancer target class for small-molecule drug discovery.
Objective:
This review discusses the patent literature of BET inhibitors (2010-2017) for the treatment of cancer and other related diseases.
Method:
BET proteins act as 'epigenetic readers' and bind to acetylated lysine residues on the tails of histones H3 and H4. Inhibition of BET proteins for a wide array of therapeutic applications has led to the discovery and development of various BET inhibitors.
Results:
The increasing significance of BET inhibitors as a potential anticancer therapeutic has led to an extensive patent activity both from academia and pharmaceutical industry. Several of the BET inhibitors are under clinical development for the treatment of various kinds of cancers.
Conclusion:
The unmet needs and challenges associated with BET inhibition for cancer treatment have been portrayed in this review. An insight into the current developments and future prospects has been described as well.
Insights
Bromodomain and Extra Terminal (BET) inhibitors show promise as cancer therapeutics. This review covers BET inhibitor patent literature from 2010-2017, highlighting clinical development for various cancers.
Area of Science:
- Epigenetics
- Pharmacology
- Oncology
Background:
- Bromodomain and Extra Terminal (BET) proteins (BRD2, BRD3, BRD4, BRDT) are emerging cancer targets.
- Small-molecule drug discovery is actively exploring BET proteins.
Purpose of the Study:
- Review patent literature on BET inhibitors from 2010-2017.
- Focus on cancer treatment and related diseases.
Main Methods:
- BET proteins function as 'epigenetic readers' binding to acetylated histones.
- Inhibition of BET proteins drives therapeutic applications and inhibitor development.
Main Results:
- Significant patent activity from academia and industry on BET inhibitors.
- Multiple BET inhibitors are in clinical development for diverse cancers.
Conclusions:
- The review addresses unmet needs and challenges in BET inhibition for cancer.
- Provides insights into current developments and future prospects of BET inhibitors.
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