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Change in enantioselectivity in bufuralol 1″-hydroxylation by the substitution of phenylalanine-120 by alanine in cytochrome P450 2D6

✍ Scribed by Kazufumi Masuda; Keietsu Tamagake; Yukie Okuda; Fumihiro Torigoe; Daisuke Tsuzuki; Takashi Isobe; Hiroyuki Hichiya; Nobumitsu Hanioka; Shigeo Yamamoto; Shizuo Narimatsu

Publisher
John Wiley and Sons
Year
2004
Tongue
English
Weight
727 KB
Volume
17
Category
Article
ISSN
0899-0042

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📜 SIMILAR VOLUMES

Roles of phenylalanine at position 120 a
Roles of phenylalanine at position 120 and glutamic acid at position 222 in the oxidation of chiral substrates by cytochrome P450 2D6
✍ Kazufumi Masuda; Keietsu Tamagake; Takashi Katsu; Fumihiro Torigoe; Keita Saito; 📂 Article 📅 2006 🏛 John Wiley and Sons 🌐 English ⚖ 350 KB

## Abstract The roles of Phe‐120 and Glu‐222 in the oxidation of chiral substrates bunitrolol (BTL) and bufuralol (BF) by CYP2D6 are discussed. Wild‐type CYP2D6 (CYP2D6‐WT) oxidized BTL to 4‐hydroxybunitrolol (4‐OH‐BTL) with substrate enantioselectivity of (__R__)‐(+)‐BTL > (__S__)‐(−)‐BTL. The sam

Enantioselectivity of bunitrolol 4-hydro
Enantioselectivity of bunitrolol 4-hydroxylation is reversed by the change of an amino acid residue from valine to methionine at position 374 of cytochrome P450-2D6
✍ Shizuo Narimatsu; Rika Kato; Toshiharu Horie; Satoshi Ono; Michio Tsutsui; Yoshi 📂 Article 📅 1999 🏛 John Wiley and Sons 🌐 English ⚖ 204 KB

The enantioselectivity of 4-hydroxylation of bunitrolol (BTL), a beta-adrenoceptor blocking drug, was studied in microsomes from human liver, human hepatoma (Hep G2) cells expressing CYP2D6, and lymphoblastoid cells expressing CYP2D6. Kinetics in human liver microsomes showed that the Vmax value for