Effect of BET inhibitors (JQ1 and RVX-208) on gene expression in HepG2 cells

ABSTRACT: Bromodomains have emerged as attractive candidates for the development of inhibitors targeting gene transcription. Inhibitors of the bromo-and-extra-terminal (BET) family recently showed promising activity in diverse disease models. However, the pleiotropic nature of BET proteins regulating tissue specific transcription has raised safety concerns and suggested that attempts should be made for domain-specific targeting. Here we report that RVX-208, a compound currently in phase II clinical trials, is a BET bromodomain inhibitor specific for second bromodomains (BD2). Co-crystal structures revealed binding modes of RVX-208 and its synthetic precursor and fluorescent recovery after photobleaching demonstrated that RVX-208 displaces BET proteins from chromatin. However, gene expression data sh

ORGANISM(S): Homo sapiens

SUBMITTER: Panagis Filippakopoulos 

PROVIDER: E-GEOD-51143 | biostudies-arrayexpress |

REPOSITORIES: biostudies-arrayexpress