High-throughput small molecule screen identifies inhibitors of aberrant chromatin accessibility.

ABSTRACT: Mutations in chromatin-modifying proteins and transcription factors are commonly associated with a wide variety of cancers. Through gain- or loss-of-function, these mutations may result in characteristic alterations of accessible chromatin, indicative of shifts in the landscape of regulatory elements genome-wide. The identification of compounds that reverse a specific chromatin signature could lead to chemical probes or potential therapies. To explore whether chromatin accessibility could serve as a platform for small molecule screening, we adapted formaldehyde-assisted isolation of regulatory elements (FAIRE), a chemical method to enrich for nucleosome-depleted genomic regions, as a high-throughput, automated assay. After demonstrating the validity and robustness of this approach, we appl

SUBMITTER: Pattenden SG 

PROVIDER: S-EPMC4801272 | biostudies-literature | 2016 Mar

REPOSITORIES: biostudies-literature