Bioorganic & medicinal chemistry

Slow-binding inhibition of 2-keto-3-deoxy-6-phosphogluconate (KDPG) aldolase

R Braga, L Hecquet, C Blonski

Index: Braga, Remi; Hecquet, Laurence; Blonski, Casimir Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 11 p. 2965 - 2972

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Citation Number: 11

Abstract

2-Keto-3-deoxy-6-phosphogluconate (KDPG) aldolase is a key enzyme in the Entner– Doudoroff pathway of bacteria. It catalyzes the reversible production of KDPG from pyruvate and d-glyceraldehyde 3-phosphate through a class I Schiff base mechanism. On the basis of aldolase mechanistic pathway, various pyruvate analogues bearing β-diketo structures were designed and synthesized as potential inhibitors. Their capacity to inhibit aldolase ...