Establishment of high throughput screening model for epidermal growth factor receptor tyrosine kinase inhibitor
文献类型：期刊论文
| 作者 | LI Lin3; LI Guo1; CHEN Li-li2 ; LUO Hai-bin2; CHEN Jing2; SHEN Xu2; MEI Chang-lin3
|
| 刊名 | Academic Journal of Second Military Medical University
 |
| 出版日期 | 2009 |
| 卷号 | 30期号:12页码:1349-1352 |
| 关键词 | epidermal growth factor receptor tyrosine kinase inhibitor model high throughout screening surface plasmon resonance |
| ISSN号 | 0258-879X |
| 其他题名 | 表皮生长因子受体酪氨酸激酶抑制剂高通量筛选模型的建立 |
| 文献子类 | Article |
| 英文摘要 | Objective:To establish a high throughput screening(HTS)model for epidermal growth factor(EGF)receptor tyrosine kinase(RTK)inhibitor.Methods:The bioactive EGFR-RTK was expressed by genetic engineering technology.The binding activity and bioactivity of the compounds were examined by surface plasmon resonance and ELISA.Results:The bioactive EGFR-RTK protein was successfully expressed in the prokaryotic expression system and was immobilized on the sensor chip.The equilibrium constants(Kd)between TKI(EI 188)and RTK was 5.00 * 10~(-7) mol·L~(-1),and the IC_(50) was 12.37mumol·L~(-1),which was consistent with expected.With this model we screened 31 compounds and found that 6 compounds had binding activity and inhibitory activity.Conclusion:A novel HTS model of EGFR-TKI has been successfully established using surface plasmon resonance biosensor and ELISA,which lays a foundation for discovery of new TKIs. |
| 资助项目 | 国家自然科学基金重点项目[00000000] ; 国家自然科学基金[00000000] ; 国家科技部重大科技专项[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:3783963 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/268021]  |
| 专题 | 生物技术药物研发中心（筹） 药物安全性评价中心 |
| 作者单位 | 1.Department of Orthopaedics,No.411 Hospital of PLA, Shanghai 200081, China.; 2.Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China. 3.Department of Nephrology,Changzheng Hospital,Second Military Medical University, Shanghai 200003, China.; |
| 推荐引用方式 GB/T 7714 | LI Lin,LI Guo,CHEN Li-li,et al. Establishment of high throughput screening model for epidermal growth factor receptor tyrosine kinase inhibitor[J]. Academic Journal of Second Military Medical University,2009,30(12):1349-1352. |
| APA | LI Lin.,LI Guo.,CHEN Li-li.,LUO Hai-bin.,CHEN Jing.,...&MEI Chang-lin.(2009).Establishment of high throughput screening model for epidermal growth factor receptor tyrosine kinase inhibitor.Academic Journal of Second Military Medical University,30(12),1349-1352. |
| MLA | LI Lin,et al."Establishment of high throughput screening model for epidermal growth factor receptor tyrosine kinase inhibitor".Academic Journal of Second Military Medical University 30.12(2009):1349-1352. |
入库方式： OAI收割
来源：上海药物研究所
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