@article{oai:kanazawa-u.repo.nii.ac.jp:00014889,
 author = {中嶋, 美紀 and 深見, 達基 and 山崎, 浩史 and Nakajima, Miki and Itoh, Masahiro and Sakai, Haruko and Fukami, Tatsuki and Kato, Miki and Yamazaki, Hiroshi and Kadlubar, Fred F. and Imaoka, Susumu and Funae, Yoshihiko and Yokoi, Tsuyoshi},
 issue = {11},
 journal = {International Journal of Cancer},
 month = {Jan},
 note = {Cigarette smoking is the predominant risk factor for bladder cancer. Aromatic amines such as 4-aminobiphenyl (ABP) is the major carcinogens found in tobacco smoke. Although it is generally accepted that ABP is metabolically activated via N-hydroxylation by CYP1A2 in human liver, previous studies using Cyp1a2-null mice indicated the involvement of other enzyme(s). Here we found that CYP2A13 can metabolically activate ABP to show genotoxicity by Umu assay. The Km and Vmax values for ABP N-hydroxylation by recombinant CYP2A13 in E. coli were 38.5 ± 0.6 μM 7.8 ± 0.0 pmol/min/pmol CYP, respectively. The Km and Vmax values by recombinant CYP1A2 were 9.9 ± 0.9 μM and 39.6 ± 0.9 pmol/min/ pmol CYP, respectively, showing 20-fold higher intrinsic clearance than CYP2A13. In human bladder, CYP2A13 mRNA, but not CYP1A2, is expressed at a relatively high level. Human bladder microsomes showed ABP N-hydroxylase activity (K m = 34.9 ± 4.7 μM and Vmax = 57.5 ± 1.9 pmol/min/mg protein), although the intrinsic clearance was 5-fold lower than that in human liver microsomes (Km = 33.2 ± 2.0 μM and Vmax = 293.9 ± 5.8 pmol/min/mg protein). The activity in human bladder microsomes was prominently inhibited by 8-methoxypsoralen, but not by fluvoxamine, anti-CYP1A2 or anti-CYP2A6 antibodies., 金沢大学ナノ生命科学研究所 / 金沢大学大学院医学系研究科機能分子医薬学 / 金沢大学薬学部},
 pages = {2520--2526},
 title = {CYP2A13 expressed in human bladder metabolically activates 4-aminobiphenyl},
 volume = {119},
 year = {2006}
}