Ontology highlight
ABSTRACT:
SUBMITTER: Xu L
PROVIDER: S-EPMC5984485 | biostudies-literature | 2018 May
REPOSITORIES: biostudies-literature
Proceedings of the National Academy of Sciences of the United States of America 20180515 22
Competitive BET bromodomain inhibitors (BBIs) targeting BET proteins (BRD2, BRD3, BRD4, and BRDT) show promising preclinical activities against brain cancers. However, the BET protein-dependent glioblastoma (GBM)-promoting transcriptional network remains elusive. Here, with mechanistic exploration of a next-generation chemical degrader of BET proteins (dBET6), we reveal a profound and consistent impact of BET proteins on E2F1- dependent transcriptional program in both differentiated GBM cells an ...[more]