Bioorganic & medicinal chemistry

A library of novel allosteric inhibitors against fructose 1, 6-bisphosphatase

S Heng, KR Gryncel, ER Kantrowitz

Index: Heng, Sabrina; Gryncel, Kimberly R.; Kantrowitz, Evan R. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 11 p. 3916 - 3922

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Citation Number: 46

Abstract

The identification of a proper lead compound for fructose 1, 6-bisphosphatase (FBPase) is a critical step in the process of developing novel therapeutics against type-2 diabetes. Herein, we have successfully generated a library of allosteric inhibitors against FBPase as potential anti-diabetic drugs, of which, the lead compound 1b was identified through utilizing a virtual high-throughput screening (vHTS) system, which we have developed. The thiazole-based ...