BET Inhibitors as Anticancer Agents: A Patent Review

Abstract

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.

Keywords: BET; BET inhibitors; BRDs; cancer; epigenetics; patent; therapeutic potential..