Inhibition of BET bromodomain targets genetically diverse glioblastoma.

ABSTRACT:

Purpose

Glioblastoma is refractory to conventional therapies. The bromodomain and extraterminal domain (BET) proteins are epigenetic readers that selectively bind to acetylated lysine residues on histone tails. These proteins recently emerged as important therapeutic targets in NUT midline carcinoma and several types of hematopoietic cancers. In this study, the therapeutic potential of a novel BET bromodomain inhibitor, JQ1, was assessed in a panel of genetically heterogeneous glioblastoma samples.

Experimental design

The antineoplastic effects of JQ1 were shown using ex vivo cultures derived from primary glioblastoma xenograft lines and surgical specimens of different genetic background. The in vivo efficacy was assessed in orthotopic glioblastoma tumors.

Results

We

SUBMITTER: Cheng Z 

PROVIDER: S-EPMC4172367 | biostudies-literature | 2013 Apr

REPOSITORIES: biostudies-literature