title: Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode.
abstract: We have identified benzoxazole benzenesulfonamide 1 as a novel allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1). X-ray crystallographic and biological studies of 1 indicate a distinct binding mode that recapitulates features of several previously reported FBPase-1 inhibitor classes.
authors.affiliation: Metabolic Disease Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064, USA. Thomas.vongeldern@abbott.com
authors.forename: Thomas W
authors.initials: TW
authors.lastname: von Geldern
authors.forename: Chunqiu
authors.initials: C
authors.lastname: Lai
authors.forename: Rebecca J
authors.initials: RJ
authors.lastname: Gum
authors.forename: Melissa
authors.initials: M
authors.lastname: Daly
authors.forename: Chaohong
authors.initials: C
authors.lastname: Sun
authors.forename: Elizabeth H
authors.initials: EH
authors.lastname: Fry
authors.forename: Celerino
authors.initials: C
authors.lastname: Abad-Zapatero
mesh_terms: D000494:Allosteric Regulation; D001583:Benzoxazoles / Q000737:chemistry*; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D006597:Fructose-Bisphosphatase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008958:Models, Molecular; D011485:Protein Binding; D013449:Sulfonamides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D001583:Benzoxazoles; D004791:Enzyme Inhibitors; D013449:Sulfonamides; D006597:Fructose-Bisphosphatase