Reversible Inhibition of Human Placental Microsomal Aromatase by CGS 18320B and Other Non-Steroidal Compounds
| Autor: | Yoshio Osawa, Dietmar G. Braun, Keith Bullion |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
Stereochemistry
Placenta Binding Competitive Endocrinology Non-competitive inhibition Pregnancy Microsomes Nitriles medicine Humans Androstenedione Aromatase Binding Sites Fadrozole Molecular Structure biology Aromatase Inhibitors Chemistry Imidazoles Aromatization Active site General Medicine Kinetics Enzyme inhibitor biology.protein Microsome Glutethimide Female Aminoglutethimide medicine.drug |
| Zdroj: | Endocrine Research. 16:255-267 |
| ISSN: | 1532-4206 0743-5800 |
| DOI: | 10.1080/07435809009033004 |
| Popis: | The effect of bis-(p-cyanophenyl)imidazo-1-yl-methane hemisuccinate (CGS 18320B) and other non-steroidal compounds on the aromatization of androstenedione by human placental microsomal aromatase was studied. CGS 18320B exhibited competitive inhibition with an apparent Ki of 0.16 nM, a 90 and 3800-fold increase in affinity compared to 4-hydroxyandrostenedione and amino-glutethimide, 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. |
| Databáze: | OpenAIRE |
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