Type I methionine aminopeptidase from Saccharomyces cerevisiae is a potential target for antifungal drug screening
文献类型：期刊论文
| 作者 | Chen, LL ; Li, J; Li, JY; Luo, QL; Mao, WF; Shen, Q; Nan, FJ; Ye, QZ
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2004-07 |
| 卷号 | 25期号:7页码:907-914 |
| 关键词 | methionine aminopeptidase high-throughput screening antifungal agent |
| ISSN号 | 1671-4083 |
| 文献子类 | Article |
| 英文摘要 | AIM: To screen antifungal drug candidates using in vitro and in vivo assays based on type I methionine aminopeptidase from Saccharomyces cerevisiae (ScMetAP1). METHODS: A colorimetric assay suitable for high throughput screening (HTS) using recombinant ScMetAP1 protein expressed in Escherichia coli was established for antifungal lead discovery. A series of pyridine-2-carboxylic acid derivatives were characterized and a chemical library of 12 800 pure organic compounds was screened with the in vitro ScMetAP1 assay. Active compounds from the in vitro assay were further evaluated by a growth inhibition assay on yeast strain with deletion of ScMetAP1 gene map1 in comparison with the wild-type yeast strain and the yeast strain with deletion of type 11 enzyme (ScMetAP2) gene map2. RESULTS: Active ScMetAP1 inhibitors were identified from HTS. Some of the pyridine-2-carboxylic acid derivatives (compound 2 and 3) had selective inhibition of the growth of map2 deletion yeast and weak inhibition on wild-type yeast growth, while no inhibition on map1 deletion yeast. CONCLUSION: ScMetAP1 is a novel potential target for developing antifungal drugs. The in vitro and in vivo ScMetAP1 assays can serve as tools in discovering antifungal drug candidates. |
| WOS关键词 | ESCHERICHIA-COLI ; PYROCOCCUS-FURIOSUS ; INHIBITORS ; FUMAGILLIN ; GENE ; OVEREXPRESSION ; PURIFICATION ; SPECIFICITY ; TRANSFERASE ; CATALYSIS |
| 资助项目 | NCRR NIH HHS[1 P20 RR15563] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000222574700009 |
| 出版者 | SHANGHAI INST MATERIA MEDICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274051]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Ye, QZ |
| 作者单位 | 1.Univ Kansas, High Throughput Screening Lab, Lawrence, KS 66047 USA 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, LL,Li, J,Li, JY,et al. Type I methionine aminopeptidase from Saccharomyces cerevisiae is a potential target for antifungal drug screening[J]. ACTA PHARMACOLOGICA SINICA,2004,25(7):907-914. |
| APA | Chen, LL.,Li, J.,Li, JY.,Luo, QL.,Mao, WF.,...&Ye, QZ.(2004).Type I methionine aminopeptidase from Saccharomyces cerevisiae is a potential target for antifungal drug screening.ACTA PHARMACOLOGICA SINICA,25(7),907-914. |
| MLA | Chen, LL,et al."Type I methionine aminopeptidase from Saccharomyces cerevisiae is a potential target for antifungal drug screening".ACTA PHARMACOLOGICA SINICA 25.7(2004):907-914. |
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。