Ontology highlight
ABSTRACT:
SUBMITTER: Tiraidis C
PROVIDER: S-EPMC2203354 | biostudies-literature | 2007 Aug
REPOSITORIES: biostudies-literature
Tiraidis Costas C Alexacou Kyra-Melinda KM Zographos Spyros E SE Leonidas Demetres D DD Gimisis Thanasis T Oikonomakos Nikos G NG
Protein science : a publication of the Protein Society 20070628 8
FR258900 has been discovered as a novel inhibitor of human liver glycogen phosphorylase a and proved to suppress hepatic glycogen breakdown and reduce plasma glucose concentrations in diabetic mice models. To elucidate the mechanism of inhibition, we have determined the crystal structure of the cocrystallized rabbit muscle glycogen phosphorylase b-FR258900 complex and refined it to 2.2 A resolution. The structure demonstrates that the inhibitor binds at the allosteric activator site, where the p ...[more]