-transparent.png){kind=logo}
Zebularine metabolism by aldehyde oxidase in hepatic cytosol from humans, monkeys, dogs, rats, and mice: influence of sex and inhibitors. 2006
Laboratory of Clinical Pharmacology, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA. klecker@cder.fda.gov
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 known potent inhibitor of AO, and 5-benzylacyclouridine (BAU), a previously undescribed inhibitor of AO. The Michaelis-Menten kinetics of aldehyde oxidase and its inhibition by raloxifene and BAU were highly variable between species.
Related Publications
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
December 2010,
Drug metabolism and disposition: the biological fate of chemicals,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
May 2021,
Biopharmaceutics & drug disposition,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
May 2011,
Xenobiotica; the fate of foreign compounds in biological systems,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
March 1999,
Drug metabolism and disposition: the biological fate of chemicals,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
January 1981,
Hormone research,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
October 1977,
Cancer treatment reports,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
April 2010,
Drug metabolism and disposition: the biological fate of chemicals,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
January 1994,
Drug metabolism and disposition: the biological fate of chemicals,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
March 1995,
Drug metabolism and disposition: the biological fate of chemicals,
Raymond W Klecker, and
Richard L Cysyk, and
Jerry M Collins
May 2014,
Drug metabolism and disposition: the biological fate of chemicals,
