Interrogating the mechanism of a tight binding inhibitor of AIR carboxylase

SM Firestine, W Wu, H Youn, VJ Davisson

Index: Firestine, Steven M.; Wu, Weidong; Youn, Hasik; Jo Davisson Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 2 p. 794 - 803

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Citation Number: 10

Abstract

The enzyme aminoimidazole ribonucleotide (AIR) carboxylase catalyzes the synthesis of the purine intermediate, 4-carboxy-5-aminoimidazole ribonucleotide (CAIR). Previously, we have shown that the compound 4-nitro-5-aminoimidazole ribonucleotide (NAIR) is a slow, tight binding inhibitor of the enzyme with a Ki of 0.34 nM. The structural attributes and the slow, tight binding characteristics of NAIR implicated this compound as a transition state or ...