BET bromodomain inhibitor HMBA synergizes with MEK inhibition in treatment of malignant glioma.

ABSTRACT: (1) Background: BET bromodomain proteins regulate transcription by binding acetylated histones and attracting key factors for, e.g., transcriptional elongation. BET inhibitors have been developed to block pathogenic processes such as cancer and inflammation. Despite having potent biological activities, BET inhibitors have still not made a breakthrough in clinical use for treating cancer. Multiple resistance mechanisms have been proposed but thus far no attempts to block this in glioma has been made. (2) Methods: Here, we have conducted a pharmacological synergy screen in glioma cells to search for possible combination treatments augmenting the apoptotic response to BET inhibitors. We first used HMBA, a compound that was developed as a differentiation therapy four decades ago but more recen

SUBMITTER: Funck-Brentano E 

PROVIDER: S-EPMC7889204 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature