基于配体结构的grb2sh2抑制剂的结构优化更高的活性更少的电荷更低的肽性
文献类型：期刊论文
| 作者 | 彭电1; 智英1; 薛婷1; 高慧媛2; 龙亚秋1 |
| 刊名 | 有机化学
 |
| 出版日期 | 2011 |
| 卷号 | 31期号:12页码:2019 |
| 关键词 | STRUCTURE-BASED DESIGN RING-CLOSING METATHESIS CONSTRAINED PHOSPHOTYROSYL MIMETICS DOMAIN-BINDING MACROCYCLES ALPHA-AMINO-ACIDS SH2 DOMAIN NONPHOSPHORYLATED INHIBITOR PHOSPHOPEPTIDE LIGANDS TYROSINE DERIVATIVES SIGNAL-TRANSDUCTION phosphotyrosine Grb2-SH2 inhibitor structure-activity relationship mitogenic ras pathway anti-tumor drug |
| ISSN号 | 0253-2786 |
| 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 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/284147]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学院上海药物研究所 2.沈阳药科大学 |
| 推荐引用方式 GB/T 7714 | 彭电,智英,薛婷,等. 基于配体结构的grb2sh2抑制剂的结构优化更高的活性更少的电荷更低的肽性[J]. 有机化学,2011,31(12):2019. |
| APA | 彭电,智英,薛婷,高慧媛,&龙亚秋.(2011).基于配体结构的grb2sh2抑制剂的结构优化更高的活性更少的电荷更低的肽性.有机化学,31(12),2019. |
| MLA | 彭电,et al."基于配体结构的grb2sh2抑制剂的结构优化更高的活性更少的电荷更低的肽性".有机化学 31.12(2011):2019. |
入库方式： OAI收割
来源：上海药物研究所
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