作者: Anastasia Wyce , Yan Degenhardt , Yuchen Bai , BaoChau Le , Susan Korenchuk
关键词: BET inhibitor 、 Oncogene 、 Biology 、 Chromatin 、 Bromodomain 、 BRD4 、 Cancer research 、 Gene expression 、 Cell growth 、 Histone
摘要: BET (bromodomain and extra-terminal) proteins regulate gene expression through their ability to bind acetylated chromatin subsequently activate RNA PolII-driven transcriptional elongation. Small molecule inhibitors prevent binding of histones inhibit activation target genes. attenuate cell growth survival in several hematologic cancer models, partially the down-regulation critical oncogene, MYC. We hypothesized that will MYC solid tumors frequently over-express Here we describe effects highly specific inhibitor, I-BET762, on prostate models. I-BET762 potently reduced lines a patient-derived tumor model with subsequent inhibition reduction burden vivo. Our data suggests are driven by underlines importance additional mechanisms induced phenotypes.