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

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

Affiliation

  • 1 Metabolic Disease Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064, USA. Thomas.vongeldern@abbott.com
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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