Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.

ABSTRACT:

Background

Acetylation of lysine residues in histone tails plays an important role in the regulation of gene transcription. Bromdomains are the readers of acetylated histone marks, and, consequently, bromodomain-containing proteins have a variety of chromatin-related functions. Moreover, they are increasingly being recognised as important mediators of a wide range of diseases. The first potent and selective bromodomain inhibitors are beginning to be described, but the diverse or unknown functions of bromodomain-containing proteins present challenges to systematically demonstrating cellular efficacy and selectivity for these inhibitors. Here we assess the viability of fluorescence recovery after photobleaching (FRAP) assays as a target agnostic method for the direct visualisation of

SUBMITTER: Philpott M 

PROVIDER: S-EPMC4115480 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature