Development of an aromatase inhibitor screening assay
文献类型：期刊论文
| 作者 | Quan Haitian ; Lou Liguang
|
| 刊名 | Chinese Pharmacological Bulletin
 |
| 出版日期 | 2004 |
| 卷号 | 20期号:10页码:1189-1192 |
| 关键词 | aromatase screening model aromatase inhibitors " tritiated water" ssay |
| ISSN号 | 1001-1978 |
| 其他题名 | 芳香化酶抑制剂筛选模型的建立 |
| 文献子类 | Article |
| 英文摘要 | Aim To develop an aromatase inhibitor screening as-say in vitro. Methods A method termed "tritiated water" assay was developed to measure aromat aseactivity by quantifying the ' H,0 from the aromatization reaction, using placental micro-somes as enzyme source and [ 1beta-3H] androstenedione as a sub-strate. Result "Tritiated water" assay was established and it was found that androstrenedione had a K_m value of 113 nmol ? L~(-1) and a V_(max) value of 33. 3 pmol ? ( min ? mg protein) "' in the aromatization reaction catalyzed by placental microsomes as determined by Lhis assay. The reliability of this assay was con-firmed by application of specific aromatase inhibitor exemestane. Exemestane was shown to be an irreversible aromatase inhibitor with the IC_(50) of 70 nmol ? L~(-1), which was comparable to find-ings by other laboratories. Conclusion These data demonstrate that " tritiated water" assay is a useful model to screen aromatase inhibitors. |
| 资助项目 | 国家重大科技专项资助项目[00000000] |
| WOS研究方向 | General & Internal Medicine ; Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:1698763 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/268379]  |
| 专题 | 药理学第一研究室 |
| 通讯作者 | Lou Liguang |
| 作者单位 | Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China. |
| 推荐引用方式 GB/T 7714 | Quan Haitian,Lou Liguang. Development of an aromatase inhibitor screening assay[J]. Chinese Pharmacological Bulletin,2004,20(10):1189-1192. |
| APA | Quan Haitian,&Lou Liguang.(2004).Development of an aromatase inhibitor screening assay.Chinese Pharmacological Bulletin,20(10),1189-1192. |
| MLA | Quan Haitian,et al."Development of an aromatase inhibitor screening assay".Chinese Pharmacological Bulletin 20.10(2004):1189-1192. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。