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  • Title: Discovery of fructose-1,6-bisphosphatase inhibitors for the treatment of type 2 diabetes.
    Author: van Poelje PD, Dang Q, Erion MD.
    Journal: Curr Opin Drug Discov Devel; 2007 Jul; 10(4):430-7. PubMed ID: 17659484.
    Abstract:
    Overproduction of glucose via gluconeogenesis is a principal cause of the high blood glucose levels found in patients with type 2 diabetes, and is inadequately controlled by currently available medications. The enzyme fructose-1,6-bisphosphatase (FBPase), a major control point in the pathway of gluconeogenesis, is recognized as an attractive target for pharmacological intervention. This review describes recent progress in the discovery and optimization of inhibitors of FBPase, with emphasis on non-competitive inhibitors that interact with the adenosine monophosphate site of the enzyme. The biological characterization of the most advanced of these drugs, CS-917, is also summarized.
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