Emerging roles of and therapeutic strategies targeting BRD4 in cancer.


Department of Surgery, Division of Surgical Oncology, The Ohio State University Wexner Medical Center and The OSU James Comprehensive Cancer Center, Columbus, OH, United States. Electronic address: [Email]


The Bromodomain and Extra-terminal (BET) family of proteins were first recognized as important epigenetic regulators in inflammatory processes; however, there is increasing evidence to support the notion that BET proteins also play a critical role in 'reading' chromatin and recruiting chromatin-regulating enzymes to control gene expression in a number of pathologic processes, including cancer. To this end, the mechanisms by which BET proteins regulate chromatin remodeling and promote tumor-associated inflammation have been heavily studied over the past decade. This article to review the biology of BET protein dysfunction in promoting tumor-associated inflammation and cancer progression and the application of small molecule inhibitors that target specific BET proteins, alone or in combination with immunomodulatory agents as a novel therapeutic strategy for cancer patients.


BET inhibitors,BRD4,Bromo- and Extra-Terminal (BET) protein family,Inflammation and cancer,

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