Ontology highlight
ABSTRACT:
SUBMITTER: Darby JF
PROVIDER: S-EPMC4501319 | biostudies-literature | 2014 Dec
REPOSITORIES: biostudies-literature
Darby John F JF Landström Jens J Roth Christian C He Yuan Y Davies Gideon J GJ Hubbard Roderick E RE
Angewandte Chemie (International ed. in English) 20141007 49
Fragment-based approaches are used routinely to discover enzyme inhibitors as cellular tools and potential therapeutic agents. There have been few reports, however, of the discovery of small-molecule enzyme activators. Herein, we describe the discovery and characterization of small-molecule activators of a glycoside hydrolase (a bacterial O-GlcNAc hydrolase). A ligand-observed NMR screen of a library of commercially available fragments identified an enzyme activator which yielded an approximate ...[more]