REVERSIBLE INHIBITION OF HUMAN PLACENTAL MICROSOMAL AROMATASE BY CGS-18320B AND OTHER NONSTEROIDAL COMPOUNDS

被引：24

作者：

BULLION, KA ^{[1
]}

OSAWA, Y ^{[1
]}

BRAUN, DG ^{[1
]}

机构：

[1] CIBA GEIGY AG,CH-4002 BASEL,SWITZERLAND

来源：

ENDOCRINE RESEARCH | 1990年 / 16卷 / 02期

关键词：

D O I：

10.1080/07435809009033004

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

The effect of bis-(p-cyanopheny1)imidazo-1-yl-methane hemisuccinate (CGS 1832OB) and other non-steroidal compounds on the aromatization of androstenedione by human placental microsomal aromatase was studied. CGS 1832OB exhibited competitive inhibition with an apparent Ki of 0.16 nM, a 90 and 3800-fold increase in affinity compared to 4-hydroxyandrostenedione and aminoglutethimide, respectively. The inhibition is not time-dependent, indicating that the active site interaction is reversible. CGS 18230B showed a two-fold increased affinity as compared to 4-5,6,7,8-tetrahydroimidazo[1,5a]pyridin-5-yl) benzonitrile (CGS 16949A) and cis-1-[(4-1-imidazoyl)methyl)cyclohexyl)methyl]-imidazole succinate (CGS 14796C) which showed Ki values of 0.35 and 0.39 4M, respectively.1-[2-(1-(4-carboxyphenyl)-3-ureido)ethyl]-2-(4-pyridyl)-2-imidazoline monohydrochloride (CGP 15720A) showed negligible inhibition. © 1990 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.

引用

页码：255 / 267

页数：13

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[2]

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[3]

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