Ontology highlight
ABSTRACT:
SUBMITTER: Lu J
PROVIDER: S-EPMC4475452 | biostudies-literature | 2015 Jun
REPOSITORIES: biostudies-literature
Chemistry & biology 20150604 6
BRD4, a bromodomain and extraterminal domain (BET) family member, is an attractive target in multiple pathological settings, particularly cancer. While BRD4 inhibitors have shown some promise in MYC-driven malignancies such as Burkitt's lymphoma (BL), we show that BRD4 inhibitors lead to robust BRD4 protein accumulation, which may account for their limited suppression of MYC expression, modest antiproliferative activity, and lack of apoptotic induction. To address these limitations we designed A ...[more]