Imran Ali 1 , Gildon Choi 1 , Kwangho Lee 1 Show Affiliations »
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Entities: Chemical
Disease
Gene
Species
Keywords:
BET; BET inhibitors; BRDs; cancer; epigenetics; patent; therapeutic potential.
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Year: 2017
PMID： 28786345 DOI： 10.2174/1574892812666170808121228
Source DB: PubMed Journal: Recent Pat Anticancer Drug Discov ISSN： 1574-8928 Impact factor: 4.169