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19-羟基-4-雄烯-17-酮:雌激素生物合成的潜在竞争性抑制剂。

19-Hydroxy-4-androsten-17-one: potential competitive inhibitor of estrogen biosynthesis.

作者信息

Numazawa M, Mutsumi A, Hoshi K, Koike R

机构信息

Tohoku College of Pharmacy, Sendai, Japan.

出版信息

Biochem Biophys Res Commun. 1989 May 15;160(3):1009-14. doi: 10.1016/s0006-291x(89)80102-0.

DOI:10.1016/s0006-291x(89)80102-0
PMID:2730636
Abstract

3-Deoxy steroids having a 4-ene system were found to be competitive inhibitors of human placental aromatase. 19-Hydroxy-4-androsten-17-one (2) potently inhibits the enzyme with an apparent Ki of 12.5 nM, but does not produce a time-dependent inactivation of the enzyme.

摘要

具有4-烯体系的3-脱氧类固醇被发现是人类胎盘芳香化酶的竞争性抑制剂。19-羟基-4-雄烯-17-酮(2)能有效抑制该酶,其表观抑制常数(Ki)为12.5 nM,但不会导致该酶的时间依赖性失活。

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19-Hydroxy-4-androsten-17-one: potential competitive inhibitor of estrogen biosynthesis.19-羟基-4-雄烯-17-酮:雌激素生物合成的潜在竞争性抑制剂。
Biochem Biophys Res Commun. 1989 May 15;160(3):1009-14. doi: 10.1016/s0006-291x(89)80102-0.
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Three-dimensional quantitative structure-activity relationships of steroid aromatase inhibitors.甾体芳香酶抑制剂的三维定量构效关系
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