Bioorganic & medicinal chemistry

Zebularine metabolism by aldehyde oxidase in hepatic cytosol from humans, monkeys, dogs, rats, and mice: influence of sex and inhibitors

RW Klecker, RL Cysyk, JM Collins

Index: Klecker, Raymond W.; Cysyk, Richard L.; Collins, Jerry M. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 1 p. 62 - 66

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Citation Number: 42

Abstract

To aid in the clinical evaluation of zebularine, a potential oral antitumor agent, we initiated studies on the metabolism of zebularine in liver cytosol from humans and other mammals. Metabolism by aldehyde oxidase (AO, EC 1.2. 3.1) was the major catabolic route, yielding uridine as the primary metabolite, which was metabolized further to uracil by uridine phosphorylase. The inhibition of zebularine metabolism was studied using raloxifene, a ...