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氨鲁米特及其代谢产物N - 乙酰氨鲁米特对牛肾上腺皮质和人胎盘细胞色素P - 450scc的影响。

Effects of aminoglutethiumide and its metabolite, N-acetylaminoglutethimide, on bovine adrenocortical and human placental cytochromes P-450scc.

作者信息

Sheets J J, Vickery L E

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Oct;321(1):70-3. doi: 10.1007/BF00586352.

DOI:10.1007/BF00586352
PMID:7144927
Abstract

The ability of aminoglutethimide to inhibit cholesterol conversion to pregnenolone was lost upon acetylation of the arylamine nitrogen. This appears to be due to failure of N-acetyl-d-aminoglutethimide to bind to cytochrome P-450scc, since it does not produce the altered low spin form of the enzyme formed upon binding of d-aminoglutethimide. These findings provide further evidence for a role of the free arenamine function in aminoglutethimide and related inhibitors.

摘要

氨鲁米特将胆固醇转化为孕烯醇酮的能力在芳胺氮乙酰化后丧失。这似乎是由于N-乙酰-d-氨鲁米特无法与细胞色素P-450scc结合,因为它不会产生在d-氨鲁米特结合后形成的酶的改变的低自旋形式。这些发现为游离芳胺功能在氨鲁米特及相关抑制剂中的作用提供了进一步的证据。

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1
Effects of aminoglutethiumide and its metabolite, N-acetylaminoglutethimide, on bovine adrenocortical and human placental cytochromes P-450scc.氨鲁米特及其代谢产物N - 乙酰氨鲁米特对牛肾上腺皮质和人胎盘细胞色素P - 450scc的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Oct;321(1):70-3. doi: 10.1007/BF00586352.
2
Inhibition of bovine adrenocortical cytochrome P-450scc by 3,3'-dimethoxybenzidine.
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[Cholesterol-hydroxylating cytochrome P-450 from bovine adrenal cortex mitochondria and human placenta: immunochemical properties and structural characteristics].[来自牛肾上腺皮质线粒体和人胎盘的胆固醇羟化细胞色素P-450:免疫化学性质和结构特征]
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Side-chain specificities of human and bovine cytochromes P-450scc.人及牛细胞色素P-450scc的侧链特异性
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10
Amino-steroids as inhibitors and probes of the active site of cytochrome P-450scc. Effects on the enzyme from different sources.氨基类固醇作为细胞色素P-450scc活性位点的抑制剂和探针。对不同来源酶的影响。
J Steroid Biochem. 1984 Feb;20(2):671-6. doi: 10.1016/0022-4731(84)90141-9.

本文引用的文献

1
THE CARBON MONOXIDE-BINDING PIGMENT OF LIVER MICROSOMES. II. SOLUBILIZATION, PURIFICATION, AND PROPERTIES.肝微粒体的一氧化碳结合色素。II. 增溶、纯化及性质
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3-Methoxybenzidine: a potent inhibitor of cholesterol side chain cleavage cytochrome P-450.
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Less toxic treatment for advanced breast cancer.晚期乳腺癌的低毒治疗方法。
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Inhibition of bovine adrenocortical cytochrome P-450scc by 3,3'-dimethoxybenzidine.
Steroids. 1981 Jan;37(1):91-101. doi: 10.1016/0039-128x(81)90011-8.
6
Proximity of the substrate binding site and the heme-iron catalytic site in cytochrome P-450scc.细胞色素P-450侧链裂解酶中底物结合位点与血红素铁催化位点的接近性。
Proc Natl Acad Sci U S A. 1982 Oct;79(19):5773-7. doi: 10.1073/pnas.79.19.5773.
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Persistent effects of a synthetic androstene derivative on activities of 3-beta-hydroxysteroid dehydrogenase and glucose-6-phosphate dehydrogenase in rats.
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The effect of steroid hydroxylase inhibitors on the rate of reduction of adrenal mitochondrial cytochrome P-450.类固醇羟化酶抑制剂对肾上腺线粒体细胞色素P-450还原速率的影响。
Biochem Biophys Res Commun. 1969 Aug 15;36(4):552-8. doi: 10.1016/0006-291x(69)90340-4.
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Cleavage of structural proteins during the assembly of the head of bacteriophage T4.在噬菌体T4头部组装过程中结构蛋白的切割
Nature. 1970 Aug 15;227(5259):680-5. doi: 10.1038/227680a0.
10
The influence of an anti-steroidogenic drug (aminoglutethimide phosphate) on pregnancy maintenance.一种抗类固醇生成药物(磷酸氨鲁米特)对维持妊娠的影响。
Endocrinology. 1972 May;90(5):1363-70. doi: 10.1210/endo-90-5-1363.