Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4.

ABSTRACT: The bromodomain and extraterminal (BET) family of proteins comprises four members-BRD2, BRD3, BRD4 and the testis-specific isoform BRDT-that largely function as transcriptional coactivators and play critical roles in various cellular processes, including the cell cycle, apoptosis, migration and invasion. BET proteins enhance the oncogenic functions of major cancer drivers by elevating the expression of these drivers, such as c-Myc in leukemia, or by promoting the transcriptional activities of oncogenic factors, such as AR and ERG in prostate cancer. Pathologically, BET proteins are frequently overexpressed and are clinically linked to various types of human cancer; they are therefore being pursued as attractive therapeutic targets for selective inhibition in patients with cancer. To this e

SUBMITTER: Dai X 

PROVIDER: S-EPMC5625299 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature