Ligand-Based Structural Optimization of Grb2-SH2 Inhibitors: High Affinity, Low Charge and Reduced Peptidic Nature
文献类型：期刊论文
| 作者 | Peng Dian2; Zhi Ying2; Xue Ting2; Gao Huiyuan1; Long Yaqiu2 |
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2011 |
| 卷号 | 31期号:12页码:2019-2033 |
| 关键词 | STRUCTURE-BASED DESIGN RING-CLOSING METATHESIS SH2 DOMAIN NONPHOSPHORYLATED INHIBITOR PHOSPHOTYROSYL MIMETICS ACID-RESIDUES BINDING ANTAGONISTS POSITION REQUIREMENTS phosphotyrosine Grb2-SH2 inhibitor structure-activity relationship mitogenic ras pathway anti-tumor drug |
| ISSN号 | 0253-2786 |
| 其他题名 | Ligand-Based Structural Optimization of Grb2-SH2 Inhibitors: High Affinity, Low Charge and Reduced Peptidic Nature |
| 英文摘要 | The growth factor receptor bound protein 2 (Grb2) is an intracellular adaptor protein. By its SH2 domain binding to the specific pTyr containing motif on the activated EGFR, Grb2 triggers the downstream activation of mitogenic Ras pathways which have been implicated in the etiology of certain breast cancers. So Grb2-SH2 has been recognized as an excellent target for the antitumor drug design. In this article, the recent progress of Grb2-SH2 inhibitors is reviewed, focused on the strategy to overcome the problems of the high charge and the low bioavailability endowed by the essential phosphotyrosine and the peptidic nature, respectively. The systematic structure-activity relationship study and the rational structural optimization were achieved based on the ligand-protein interaction to improve the potency and simplify the molecular structure, providing useful information for the future development of phosphotyrosine-mediated SH2 signaling inhibitors into antitumor agents. |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4413751 |
| 源URL | [http://ir.imr.ac.cn/handle/321006/153849]  |
| 专题 | 金属研究所_中国科学院金属研究所 |
| 作者单位 | 1.中国科学院金属研究所 2.中国科学院 |
| 推荐引用方式 GB/T 7714 | Peng Dian,Zhi Ying,Xue Ting,et al. Ligand-Based Structural Optimization of Grb2-SH2 Inhibitors: High Affinity, Low Charge and Reduced Peptidic Nature[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2011,31(12):2019-2033. |
| APA | Peng Dian,Zhi Ying,Xue Ting,Gao Huiyuan,&Long Yaqiu.(2011).Ligand-Based Structural Optimization of Grb2-SH2 Inhibitors: High Affinity, Low Charge and Reduced Peptidic Nature.CHINESE JOURNAL OF ORGANIC CHEMISTRY,31(12),2019-2033. |
| MLA | Peng Dian,et al."Ligand-Based Structural Optimization of Grb2-SH2 Inhibitors: High Affinity, Low Charge and Reduced Peptidic Nature".CHINESE JOURNAL OF ORGANIC CHEMISTRY 31.12(2011):2019-2033. |
入库方式： OAI收割
来源：金属研究所
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。