William F Bosron

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Capecitabine is an oral prodrug of 5-fluorouracil that is indicated for the treatment of breast and colorectal cancers. A three-step in vivo-targeted activation process requiring carboxylesterases, cytidine deaminase, and thymidine phosphorylase converts capecitabine to 5-fluorouracil. Carboxylesterases hydrolyze capecitabine's carbamate side chain to form(More)
Purified human liver carboxylesterase (hCE-1) catalyzes the hydrolysis of cocaine to form benzoylecgonine, the deacetylation of heroin to form 6-acetylmorphine, and the ethanol-dependent transesterification of cocaine to form cocaethylene. In this study, the binding affinities of cocaine, cocaine metabolites and analogs, heroin, morphine, and(More)
Carboxylesterases metabolize ester, thioester, carbamate, and amide compounds to more soluble acid, alcohol, and amine products. They belong to a multigene family with about 50% sequence identity between classes. CES1A1 and CES2 are the most studied human isoenzymes from class 1 and 2, respectively. In this study, we report the cloning and expression of a(More)
The stimulant effects of cocaine are relatively short lived, as evidenced by the increase in heart rate that peaks at about 60 minutes after cocaine administration and declines thereafter (Farre et al. 1993). This duration of effect is largely due to the rapid hydrolysis of cocaine to two major deesterified metabolites that appear in serum and urine,(More)
Since alcohol dehydrogenase (ADH) catalyzes the rate-limiting step for ethanol metabolism, knowledge of the steady-state kinetics of ADH in liver is fundamental to the understanding of the pharmacokinetics of ethanol elimination. Accordingly, we have determined the kinetic properties of purified ADH isoenzymes in rat and human liver. At low ethanol(More)
Abuse of cocaine in combination with other drugs is a widespread practice (Washton and Gold 1987) and the coabuse of alcohol is particularly common, with 99 percent of cocaine addicts reporting excessive use of ethanol in one study (Newcombe and Bentler 1987). Simultaneous ingestion of ethanol also is common, as reported by 77 percent of cocaine users(More)
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