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1-甲基-1,4-雄甾二烯-3,17-二酮(SH 489):一种雌激素生物合成不可逆抑制剂的特性研究

1-Methyl-1,4-androstadiene-3,17-dione (SH 489): characterization of an irreversible inhibitor of estrogen biosynthesis.

作者信息

Henderson D, Norbisrath G, Kerb U

出版信息

J Steroid Biochem. 1986 Jan;24(1):303-6. doi: 10.1016/0022-4731(86)90069-5.

DOI:10.1016/0022-4731(86)90069-5
PMID:3754599
Abstract

1-Methyl-1,4-androstadiene-3,17-dione (SH 489) was characterized as a competitive and irreversible inhibitor of human placental aromatase. The compound and the principal predicted metabolites show no endocrinological side effects suggesting that SH 489 should be suitable as a prototype drug for treatment of estrogen-dependent disease states.

摘要

1-甲基-1,4-雄甾二烯-3,17-二酮(SH 489)被鉴定为人类胎盘芳香化酶的竞争性不可逆抑制剂。该化合物及其主要预测代谢产物未显示出内分泌副作用,这表明SH 489应适合作为治疗雌激素依赖性疾病状态的原型药物。

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1
1-Methyl-1,4-androstadiene-3,17-dione (SH 489): characterization of an irreversible inhibitor of estrogen biosynthesis.1-甲基-1,4-雄甾二烯-3,17-二酮(SH 489):一种雌激素生物合成不可逆抑制剂的特性研究
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Androst-5-ene-7,17-dione: a novel class of suicide substrate of aromatase.雄甾-5-烯-7,17-二酮:一种新型的芳香化酶自杀底物。
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Biol Pharm Bull. 2006 Jun;29(6):1242-5. doi: 10.1248/bpb.29.1242.

引用本文的文献

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Steroids. 2007 Jan;72(1):7-25. doi: 10.1016/j.steroids.2006.10.009. Epub 2006 Dec 13.
2
Inhibitors of aromatase prevent degradation of the enzyme in cultured human tumour cells.芳香化酶抑制剂可防止培养的人肿瘤细胞中该酶的降解。
Br J Cancer. 1998 Feb;77(4):567-72. doi: 10.1038/bjc.1998.92.
3
Metabolism of the steroidal aromatase inhibitor atamestane in rats, cynomolgus monkeys and humans. Isolation and identification of the major metabolites.
甾体芳香化酶抑制剂阿他美坦在大鼠、食蟹猴和人类中的代谢。主要代谢产物的分离与鉴定。
Eur J Drug Metab Pharmacokinet. 1994 Apr-Jun;19(2):137-50. doi: 10.1007/BF03188834.
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Breast Cancer Res Treat. 1994;30(1):31-42. doi: 10.1007/BF00682739.
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Cancer Chemother Pharmacol. 1989;23(1):47-50. doi: 10.1007/BF00258457.