Inactivation of hamster monomorphic N-acetyltransferase by vinyl fluorenyl ketone.
Arylamine N-acetyltransferases (NATs) are cytosolic enzymes that play important roles in the detoxification and activation of xenobiotic arylamines and their metabolites. Vinyl fluorenyl ketone (VFK) is a selective and potent active site-directed irreversible inhibitor of rat liver monomorphic NAT. The present study demonstrated that VFK is an active site-directed affinity label for hamster liver monomorphic NAT, but is a much less effective inactivator of the polymorphic N-acetyltransferase isozyme. The potency, irreversibility and selectivity of VFK make it a potentially valuable tool for characterization of NATs that exhibit acetyl donor specificity similar to that of hamster monomorphic NAT.
Department of Pharmacology, University of Minnesota, Minneapolis 55455.
M J
MJ
Wick
P E
PE
Hanna
D000345:Affinity Labels; D000818:Animals; D001191:Arylamine N-Acetyltransferase / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D001665:Binding Sites; D006224:Cricetinae; D005449:Fluorenes / Q000494:pharmacology*; D008099:Liver / Q000201:enzymology*; D008297:Male; D008647:Mesocricetus
D000345:Affinity Labels; D005449:Fluorenes; C065765:1-(fluoren-2-yl)-2-propen-1-one; D001191:Arylamine N-Acetyltransferase