文章基本信息

标题：Mechanism of Inhibition of Carbonyl Reductase from Rabbit Kidney by Phenylbutazone
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作者：Toshiyuki HIGUCHI ; Yorishige IMAMURA ; Masaki OTAGIRI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1995
卷号：18
期号：4
页码：618-620
DOI：10.1248/bpb.18.618
出版社：The Pharmaceutical Society of Japan
摘要：Phenylbutazone showed significant inhibition against the metabolic reduction of acetohexamide catalyzed by carbonyl reductase purified from rabbit kidney. Thus, the inhibitory effect of phenylbutazone was kinetically examined. Phenylbutazone was a competitive inhibitor for the enzyme with respect to NADPH, whereas it noncompetitively inhibited the enzyme activity with respect to acetohexamide. A fluorescence study revealed that phenylbutazone decreases the binding of NADPH to the free enzyme (apoenzyme). These results suggest that phenylbutazone causes the inhibition of carbonyl reductase by competing with NADPH in its coenzyme-binding domain.
关键词：carbonyl reductase;rabbit kidney;acetohexamide reduction;phenylbutazone;inhibition mechanism