R132H IDH1 sensitizes glioma to the antiproliferative and cytotoxic effects of BET inhibition.

ABSTRACT:

Introduction

Mutations in isocitrate dehydrogenase 1/2 (IDH^mut) identify a subset of gliomas that exhibit epigenetic dysregulation via aberrant DNA methylation. These tumors are ultimately fatal and lack effective therapeutic strategies. Considering the epigenetic dysregulation of IDH^mut gliomas, we hypothesized that epigenetic-targeting drugs may yield therapeutic benefits in gliomas bearing IDH^mut. One set of targets includes the bromodomain and extraterminal (BET) family of transcriptional coactivators.

Methods

We used TCGA data from glioma patients to determine whether BET proteins affect patient survival differently based on IDH status. Follow-up experiments using a set of IDH wildtype/mutant glioma cultures, as well as an IDH wildtype g

SUBMITTER: Sears TK 

PROVIDER: S-EPMC9349147 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature