Ontology highlight
ABSTRACT:
SUBMITTER: Vazquez-Rodriguez S
PROVIDER: S-EPMC6391970 | biostudies-literature | 2019 Jan
REPOSITORIES: biostudies-literature
Angewandte Chemie (International ed. in English) 20181207 2
Histone lysine demethylases (KDMs) are involved in the dynamic regulation of gene expression and they play a critical role in several biological processes. Achieving selectivity over the different KDMs has been a major challenge for KDM inhibitor development. Here we report potent and selective KDM5 covalent inhibitors designed to target cysteine residues only present in the KDM5 sub-family. The covalent binding to the targeted proteins was confirmed by MS and time-dependent inhibition. Addition ...[more]