Design, synthesis, and evaluation of inhibitors of pyruvate phosphate dikinase

…, D Dunaway-Mariano, PS Mariano

Index: Wu, Chun; Dunaway-Mariano, Debra; Mariano, Patrick S. Journal of Organic Chemistry, 2013 , vol. 78, # 5 p. 1910 - 1922

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Citation Number: 5

Abstract

Pyruvate phosphate dikinase (PPDK) catalyzes the phosphorylation reaction of pyruvate that forms phosphoenolpyruvate (PEP) via two partial reactions: PPDK+ ATP+ Pi→ PPDK-P+ AMP+ PPi and PPDK-P+ pyruvate→ PEP+ PPDK. Based on its role in the metabolism of microbial human pathogens, PPDK is a potential drug target. A screen of substances that bind to the PPDK ATP-grasp domain active site revealed that flavone analogues are ...