Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode.
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.
von Geldern
Thomas W
TW
Metabolic Disease Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064, USA. Thomas.vongeldern@abbott.com
Lai
Chunqiu
C
Gum
Rebecca J
RJ
Daly
Melissa
M
Sun
Chaohong
C
Fry
Elizabeth H
EH
Abad-Zapatero
Celerino
C
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*
D001583:Benzoxazoles; D004791:Enzyme Inhibitors; D013449:Sulfonamides; D006597:Fructose-Bisphosphatase