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Name Koyanagi Junichi
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Title

A metabolic pathway for the prodrug nabumetone to the pharmacologically active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA) by non-cytochrome P450 enzymes 

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Summary

Nabumetone has recently been proposed as a typical substrate of flavin-containing 
monooxygenase isoform 5 (FMO5) and was shown to be efficiently oxidized in vitro
to 6-MNEA. 6-MNA was detected in the extract obtained from a combined incu-
bation of recombinant FMO5 and S9 fractions.
The specificity of FMO5 towards catalyzing this Baeyer-Villiger oxidation (BVO)
was demonstrated by the inhibition of the BVO substrate, 4-methoxyphenylacetone.
Further in vitro inhibition studies demonstrated that multiple non-cytochrome P450
enzymes are involved in the formation of 6-MNA.

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Xenobiotica, 50, 783-792 (2020)

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2020/04

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International Journal

 

International Collaboration

 

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Download

 

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