Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction
文献类型：期刊论文
| 作者 | Chen, Danqi1 ; Chen, Yuehong2; Lian, Fulin1; Chen, Liu1; Li, Yanlian1; Cao, Danyan1; Wang, Xin1; Chen, Lin1; Li, Jian1; Meng, Tao1
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| 刊名 | European journal of medicinal chemistry
 |
| 出版日期 | 2018-12-11 |
| 卷号 | 163页码:597-609 |
| ISSN号 | 1768-3254 |
| DOI | 10.1016/j.ejmech.2018.12.018 |
| 文献子类 | Article |
| 英文摘要 | Although mutated Ras protein is well recognized as an important drug target, direct targeting Ras has proven to be a daunting task. Recent studies demonstrated that Ras protein needs PDEδ to relocate to plasma membrane to execute its signaling transduction function, which provides a new avenue for modulating the Ras protein. To find small molecules antagonizing the interactions between PDEδ and Ras, here we presented a successful application of fragment-based drug discovery of PDEδ inhibitors. Under the guidance of crystal structures, we are able to quickly optimize the initial fragment into highly potent inhibitors, with more than 2000-fold improvement in binding activity, which further adds to the arsenal towards the inhibition of Ras signaling in cancer therapy. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266256]  |
| 专题 | 药理学第一研究室 分析化学研究室 药物化学研究室 |
| 通讯作者 | Huang, Min; Zhang, Naixia; Xiong, Bing |
| 作者单位 | 1.Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai, 201203, China; 2.Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai, 201203, China |
| 推荐引用方式 GB/T 7714 | Chen, Danqi,Chen, Yuehong,Lian, Fulin,et al. Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction[J]. European journal of medicinal chemistry,2018,163:597-609. |
| APA | Chen, Danqi.,Chen, Yuehong.,Lian, Fulin.,Chen, Liu.,Li, Yanlian.,...&Xiong, Bing.(2018).Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction.European journal of medicinal chemistry,163,597-609. |
| MLA | Chen, Danqi,et al."Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction".European journal of medicinal chemistry 163(2018):597-609. |
入库方式： OAI收割
来源：上海药物研究所
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