title: Inhibition of D-3-aminoisobutyrate-pyruvate aminotransferase by 5-fluorouracil and alpha-fluoro-beta-alanine.
abstract: Among pyrimidine derivatives, we found that 5-fluorouracil potently inhibited purified rat liver D-3-aminoisobutyrate-pyruvate aminotransferase, whereas 5-fluorouridine did so to a much lesser extent. 5-Fluorouracil acted as a competitive inhibitor against beta-alanine with a Ki of 56 microM, and was uncompetitive against pyruvic acid, with a Ki of 73 microM. alpha-Fluoro-beta-alanine, a metabolite of 5-fluorouracil, was also a competitive inhibitor with respect to beta-alanine with a Ki of 8.0 mM. 5-Fluorouracil acted also as a competitive inhibitor of 4-aminobutyrate aminotransferase with respect to beta-alanine with a Ki value of 1.9 mM, and was uncompetitive against 2-oxoglutaric acid, with a Ki of 1.8 mM.
authors.affiliation: Faculty of Nutrition, Kobe-Gakuin University, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Kaneko
authors.forename: Y
authors.initials: Y
authors.lastname: Kontani
authors.forename: M
authors.initials: M
authors.lastname: Kikugawa
authors.forename: N
authors.initials: N
authors.lastname: Tamaki
mesh_terms: D000410:Alanine Transaminase / Q000037:antagonists & inhibitors; D000818:Animals; D005472:Fluorouracil / Q000494:pharmacology*; D007700:Kinetics; D008099:Liver / Q000201:enzymology; D051381:Rats; D013941:Thymine / Q000031:analogs & derivatives; D000637:Transaminases / Q000037:antagonists & inhibitors*; D015091:beta-Alanine / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D015091:beta-Alanine; C032348:alpha-fluoro-beta-alanine; D000637:Transaminases; D000410:Alanine Transaminase; C019685:D-3-aminoisobutyrate-pyruvate aminotransferase; D013941:Thymine; D005472:Fluorouracil