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- W2072456719 abstract "The leucine 211 → phenylalanine (L211F) and leucine 211 → tyrosine (L211Y) mutant forms of cytochrome P450 3A4 have been generated by site-directed mutagenesis and expressed functionally in<i>Escherichia coli</i>. Substrate binding affinities (S<sub>50</sub> values) for testosterone and 7-benzyloxy-4-trifluoromethylcoumarin (BFC) were similar for the mutants and wild-type CYP3A4 (49 and 21 μM for L211F, 35 and 20 μM for L211Y, and 33 and 20 μM for the wild type, respectively). For erythromycin, however, the <i>K</i><sub>m</sub> values determined for the L211F and L211Y mutants were 2.4- and 10.5-fold higher than for the wild type. Furthermore, IC<sub>50</sub> values for the inhibition of testosterone 6β-hydroxylation by erythromycin and troleandomycin for L211F were 2.4- and 3.7-fold higher, and those for L211Y were 3.4- and 9.2-fold higher than those measured for the wild type. Conversely, small inhibitors, such as diazepam, exhibited no significant difference in IC<sub>50</sub> values between the wild type and the L211F and L211Y mutants. It is proposed that large substrates bound in the catalytic center of CYP3A4 with molecular volumes greater than ∼600 Å<sup>3</sup> were less well accommodated in the altered active sites, resulting in lower association energies and increased IC<sub>50</sub> values." @default.
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- W2072456719 date "2002-04-01" @default.
- W2072456719 modified "2023-09-27" @default.
- W2072456719 title "CYP3A4 Active Site Volume Modification by Mutagenesis of Leucine 211" @default.
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- W2072456719 doi "https://doi.org/10.1124/dmd.30.4.452" @default.
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