Article
Metabolism of N-substituted 7-methoxy-4-(aminomethyl) -coumarins by cytochrome P450 2D6 mutants and the indication of additional substrate interaction points.
Xenobiotica; the fate of foreign compounds in biological systems - 1 Sept 2006
Keizers P H J, Van Dijk B R, De Graaf C, Van Vugt-Lussenburg B M A, Vermeulen N P E, Commandeur J N M
Abstract excerpt
Previous studies have shown the critical roles residues F120 and F483 play in the oxidative metabolism of 7-methoxy-4-(aminomethyl)-coumarin (MAMC) by cytochrome P450 2D6 (CYP2D6). In the present study, a series of N-alkyl-7-methoxy-4-(aminomethyl)-coumarins (MAMC analogues) were used as substrates for the F120A and F483A mutants in order to probe the CYP2D6 active site. The F120A and F483A mutants of CYP2D6...
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