Article
Alteration of the function of the UDP-glucuronosyltransferase 1A subfamily by cytochrome P450 3A4: different susceptibility for UGT isoforms and UGT1A1/7 variants.
Drug metabolism and disposition: the biological fate of chemicals - 1 Feb 2014
Ishii Yuji, Koba Hiroki, Kinoshita Kousuke, Oizaki Toshiya, Iwamoto Yuki, Takeda Shuso, Miyauchi Yuu, Nishimura Yoshio, Egoshi Natsuki, Taura Futoshi, Morimoto Satoshi, Ikushiro Shin'ichi, Nagata Kiyoshi, Yamazoe Yasushi, Mackenzie Peter I, Yamada Hideyuki
Abstract excerpt
Functional protein-protein interactions between UDP-glucuronosyltransferase (UGT)1A isoforms and cytochrome P450 (CYP)3A4 were studied. To this end, UGT1A-catalyzed glucuronidation was assayed in Sf-9 cells that simultaneously expressed UGT and CYP3A4. In the kinetics of UGT1A6-catalyzed glucuronidation of serotonin, both Michaelis constant (Km) and maximal velocity (Vmax) were increased by CYP3A4. When CYP3A4...
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