Ontology highlight
ABSTRACT:
SUBMITTER: Stuckey JI
PROVIDER: S-EPMC4755828 | biostudies-literature | 2016 Mar
REPOSITORIES: biostudies-literature
Nature chemical biology 20160125 3
We report the design and characterization of UNC3866, a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. Polycomb CBX proteins regulate gene expression by targeting Polycomb repressive complex 1 (PRC1) to sites of H3K27me3 via their chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains whil ...[more]