Ontology highlight
ABSTRACT:
SUBMITTER: Bowler JM
PROVIDER: S-EPMC3840467 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Bowler Joseph M JM Hervert Katherine L KL Kearley Mark L ML Miller Brian G BG
ACS medicinal chemistry letters 20130901 7
Synthetic allosteric activators of human glucokinase are receiving considerable attention as potential diabetes therapeutic agents. Although their mechanism of action is not fully understood, structural studies suggest that activator association requires prior formation of a binary enzyme-glucose complex. Here, we demonstrate that three previously described activators associate with glucokinase in a glucose-independent fashion. Transient-state kinetic assays reveal a lag in enzyme progress curve ...[more]