Ontology highlight
ABSTRACT:
SUBMITTER: Xu L
PROVIDER: S-EPMC5984485 | biostudies-literature | 2018 May
REPOSITORIES: biostudies-literature
Xu Liang L Chen Ye Y Mayakonda Anand A Koh Lynnette L Chong Yuk Kien YK Buckley Dennis L DL Sandanaraj Edwin E Lim See Wee SW Lin Ruby Yu-Tong RY Ke Xin-Yu XY Huang Mo-Li ML Chen Jianxiang J Sun Wendi W Wang Ling-Zhi LZ Goh Boon Cher BC Dinh Huy Q HQ Kappei Dennis D Winter Georg E GE Ding Ling-Wen LW Ang Beng Ti BT Berman Benjamin P BP Bradner James E JE Tang Carol C Koeffler H Phillip HP
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]