The metabolism of environmentally occurring methylated polynuclear aromatic hydrocarbons by human cytochrome P450 (P450) enzymes has not been examined previously. We compared the metabolism of the tobacco smoke constituents 5-methylchrysene (5-MeC), a strong carcinogen, and 6-MeC, a weak carcinogen, in 18 hepatic and 11 pulmonary human microsomes. Major metabolites of 5-MeC were its proximate c...

O(6)-Benzylguanine (BG) effectively inactivates the DNA repair protein O(6)-alkylguanine-DNA alkyltransferase and enhances the effectiveness of alkylating agents, such as 1,3-bis(2-chloroethyl)-1-nitrosourea and temozolomide, in vitro and in vivo. BG is presently in clinical trials with 1,3-bis(2-chloroethyl)-1-nitrosourea and temozolomide. Preclinical data demonstrate that BG enhances the sens...

O-Benzylguanine (BG) effectively inactivates the DNA repair protein O-alkylguanine-DNA alkyltransferase and enhances the effectiveness of alkylating agents, such as 1,3bis(2-chloroethyl)-1-nitrosourea and temozolomide, in vitro and in vivo. BG is presently in clinical trials with 1,3-bis(2chloroethyl)-1-nitrosourea and temozolomide. Preclinical data demonstrate that BG enhances the sensitivity ...

Eight inhibitory monoclonal antibodies (MAbs) individually specific to human cytochrome P-450 (P-450) 1A1, 1A2, 2A6, 2B6, 2C subfamily (2C8, 2C9, 2C18 and 2C19), 2D6, 2E1, and 3A4/5 were used to define the role of single P-450s in the metabolism of diazepam (DZ), 7-ethoxycoumarin (7-EC), and imipramine (IMI) in human liver microsomes (HLM). The MAbs were added combinatorially to six HLM samples...

a Department of Philosophy, Carnegie Mellon University, Pittsburgh, PA 15213, USA b Center for Causal Discovery, University of Pittsburgh – Carnegie Mellon University, Pittsburgh, PA 15206, USA c Department of Psychology, Center for Learning and Memory, Institute for Neuroscience, University of Texas at Austin, Austin, TX 78712, USA * Present address: Department of Psychology, University of Tor...

McGill University Health Centre, Royal Victoria Hospital, Montreal, Quebec Correspondence: Dr Peter TK Chan, McGill University Health Centre, Royal Victoria Hospital, Department of Urology, S 6.95, 687 Pine Avenue West, Montreal, Quebec H3A 1A1. Telephone 514-842-1231 ext 34808, fax 514-843-1552, e-mail [email protected] PTK Chan. Azoospermia – Evaluations and treatments. J Sex Reprod...

Mycophenolic acid (MPA; 1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzylfuranyl)-4-methyl-4-hexenoate), the active metabolite of the immunosuppressant prodrug, mycophenolate mofetil, undergoes glucuronidation to its 7-O-glucuronide as a primary route of metabolism. Because differences in glucuronidation may influence the efficacy and/or toxicity of MPA, we investigated the MPA UDP-glu...