Ontology highlight
ABSTRACT:
SUBMITTER: Meier JC
PROVIDER: S-EPMC5662925 | biostudies-literature | 2017 Oct
REPOSITORIES: biostudies-literature
ACS chemical biology 20170912 10
Histone acetyltransferases of the MYST family are recruited to chromatin by BRPF scaffolding proteins. We explored functional consequences and the therapeutic potential of inhibitors targeting acetyl-lysine dependent protein interaction domains (bromodomains) present in BRPF1-3 in bone maintenance. We report three potent and selective inhibitors: one (PFI-4) with high selectivity for the BRPF1B isoform and two pan-BRPF bromodomain inhibitors (OF-1, NI-57). The developed inhibitors displaced BRPF ...[more]