TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) is a tight binding inhibitor of cytochrome P-450d.
TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) is a tight binding inhibitor of cytochrome P-450d.
复制标题
TCDD（2,3,7,8-四氯二苯并-对-二恶英）是细胞色素 P-450d 的紧密结合抑制剂。
DOI：
10.1002/jbt.2570040206
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发表时间：
1989
期刊：
影响因子：
--
通讯作者：
Aust,SD
中科院分区：
文献类型：
--
作者：
Voorman,R;Aust,SD
Based on data indicating that compounds which induce cytochrome P-450d also bind to the enzyme (R. Voorman and SD Aust (1987). Toxicol. Appl. Pharmacol. 90,[69–78], we investigated the inhibition of cytochrome P-450d-dependent estradiol 2-hydroxylase by (2, 3, 7, 8-tetrachlorodibenzo-p-dioxin TCDD), using ligand-free cytochrome P-450d from isosafrole-treated rats. Since maximum inhibition of estradiol 2-hydroxylase occurred at TCDD concentrations comparable to the concentration of enzyme (50 nM), a modified form of steady-state kinetic analysis was used. Using I50= E t/2+ K i where E t= total enzyme concentration), we showed that TCDD inhibited cytochrome P-450d-dependent estradiol 2-hydroxylase activity with K i equal to 8 nM. Association of TCDD with P-450d occurred within 2 min of inhibitor addition. Therefore, TCDD can be considered a tight binding inhibitor of cytochrome P-450d.
