The MAPK Pathway Regulates Intrinsic Resistance to BET Inhibitors in Colorectal Cancer.

ABSTRACT: Purpose: The bromodomain and extra-terminal domain (BET) family proteins are epigenetic readers for acetylated histone marks. Emerging BET bromodomain inhibitors have exhibited antineoplastic activities in a wide range of human cancers through suppression of oncogenic transcription factors, including MYC. However, the preclinical activities of BET inhibitors in advanced solid cancers are moderate at best. To improve BET-targeted therapy, we interrogated mechanisms mediating resistance to BET inhibitors in colorectal cancer.Experimental Design: Using a panel of molecularly defined colorectal cancer cell lines, we examined the impact of BET inhibition on cellular proliferation and survival as well as MYC activity. We further tested the ability of inhibitors targeting the RAF/ME

SUBMITTER: Ma Y 

PROVIDER: S-EPMC5368030 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature