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Stereoselective S-oxidation of flosequinan sulfide by rat hepatic flavin-containing monooxygenase 1A1 expressed in yeast.
- Source :
-
Biochemical pharmacology [Biochem Pharmacol] 1994 Apr 20; Vol. 47 (8), pp. 1357-63. - Publication Year :
- 1994
-
Abstract
- Rat hepatic flavin-containing monooxygenase (FMO) 1A1 expressed in yeast catalysed the S-oxidation of flosequinan sulfide (7-fluoro-1-methyl-3-methylthio-4-quinolone) to R(+)-flosequinan (sulfoxide form, R(+)-7-fluoro-1-methyl-3-methylsulfinyl-4-quinolone) but not to S(-)-flosequinan, and did not catalyse the oxidation of R(+)- and S(-)-flosequinan to flosequinan sulfone. The Km and Vmax for the stereoselective S-oxidation were 33 microM and 6.2 nmol per min per mg of microsomal protein, respectively. The S-oxidation was inhibited by 1-(1-naphthyl)-2-thiourea and thiobenzamide. n-Octylamine activated the S-oxidation with little change in stereoselectivity. The ability of the recombinant yeast to produce R(+)-flosequinan from flosequinan sulfide could be maintained for at least 2 days and exemplifies the value of a recombinant yeast expressing FMO as a stereoselective bioreactor.
Details
- Language :
- English
- ISSN :
- 0006-2952
- Volume :
- 47
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Biochemical pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 8185644
- Full Text :
- https://doi.org/10.1016/0006-2952(94)90334-4