Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode

  • Bioorg Med Chem Lett. 2006 Apr 1;16(7):1811-5. doi: 10.1016/j.bmcl.2006.01.015.
Thomas W von Geldern  1 ,  Chunqiu Lai ,  Rebecca J Gum ,  Melissa Daly ,  Chaohong Sun ,  Elizabeth H Fry ,  Celerino Abad-Zapatero
Affiliations
  • 1. Metabolic Disease Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064, USA. [email protected]
PMID: 16442285 DOI: 10.1016/j.bmcl.2006.01.015
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.

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