Progress of anti-tumor study based on BRAF
文献类型：期刊论文
| 作者 | Yan Guirui; Xu Zhijian ; Wang Heyao; Zhu Weiliang
|
| 刊名 | Acta Pharmaceutica Sinica
 |
| 出版日期 | 2012 |
| 卷号 | 47期号:12页码:1567-1574 |
| 关键词 | BRAF BRAF target anti-tumor |
| ISSN号 | 0513-4870 |
| 其他题名 | 基于靶标BRAF的抗肿瘤研究进展 |
| 文献子类 | Review |
| 英文摘要 | BRAF is one of the most important pro-oncogenes, which is mutated in approximately 8% of human tumors. The most common BRAF mutation is a valine-to-glutamate transition (V600E) that is expressed primarily in melanoma, colorectal cancer and thyroid carcinoma. MEK/ERK is constitutively activated in the cells expressing BRAFV600E, leading to tumor development, invasion,and metastasis. Therefore, BRAFV600E is a therapeutic target for melanoma and some other BRAFV600E tumors. Vemurafenib,a BRAFV600E inhibitor, which was approved by FDA for the treatment of late-stage melanoma in 2011,produces improved rates of overall and progression-free survival in patients with the BRAFV600E mutation,making a dramatic breakthrough in melanoma treatment. Vemurafenib is also an individual target drug based on genetic diagnosis. However, its therapeutic success is limited by the emergence of drug resistance. Therefore, it is important to explore the mechanisms underlying the resistance for developing new inhibitor drugs and for preventing or delaying the resistance evolution to BRAF inhibitor drugs. In this review, we described the role of BRAFV600E as an anti-tumor drug target and the development of BRAF inhibitors. We also discussed the mechanisms leading to resistance of BRAFV600E inhibitors. Furthermore, therapeutic strategies that might be employed to overcome acquired resistance were proposed. |
| 资助项目 | 上海市生物医药重点科技攻关项目[00000000] ; 国家重大新药创制项目[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:4719582 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/267805]  |
| 专题 | 药物发现与设计中心 |
| 通讯作者 | Zhu Weiliang |
| 作者单位 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. |
| 推荐引用方式 GB/T 7714 | Yan Guirui,Xu Zhijian,Wang Heyao,et al. Progress of anti-tumor study based on BRAF[J]. Acta Pharmaceutica Sinica,2012,47(12):1567-1574. |
| APA | Yan Guirui,Xu Zhijian,Wang Heyao,&Zhu Weiliang.(2012).Progress of anti-tumor study based on BRAF.Acta Pharmaceutica Sinica,47(12),1567-1574. |
| MLA | Yan Guirui,et al."Progress of anti-tumor study based on BRAF".Acta Pharmaceutica Sinica 47.12(2012):1567-1574. |
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。