INHIBITION OF D-3-AMINOISOBUTYRATE PYRUVATE AMINOTRANSFERASE BY 5-FLUOROURACIL AND ALPHA-FLUORO-BETA-ALANINE

被引:8
作者
KANEKO, M [1 ]
KONTANI, Y [1 ]
KIKUGAWA, M [1 ]
TAMAKI, N [1 ]
机构
[1] KOBE GAKUIN UNIV,FAC NUTR,NISHI KU,KOBE 65121,JAPAN
关键词
D-3-AMINOISOBUTYRATE PYRUVATE AMINOTRANSFERASE; 5-FLUOROURACIL; ALPHA-FLUORO-BETA-ALANINE; D-3-AMINOISOBUTYRATE; BETA-ALANINE; 4-AMINOBUTYRATE AMINOTRANSFERASE; (RAT);
D O I
10.1016/0167-4838(92)90125-W
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 K(i) of 56-mu-M, and was uncompetitive against pyruvic acid, with a K(i) of 73-mu-M. Alpha-Fluoro-beta-alanine, a metabolite of 5-fluorouracil, was also a competitive inhibitor with respect to beta-alanine with a K(i) of 8.0 mM. 5-Fluorouracil acted also as a competitive inhibitor of 4-aminobutyrate aminotransferase with respect to beta-alanine with a K(i) value of 1.9 mM, and was uncompetitive against 2-oxoglutaric acid, with a K(i) of 1.8 mM.
引用
收藏
页码:45 / 49
页数:5
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