Identification and characterization of small molecule inhibitors of signal transducer and activator of transcription 3 (STAT3) signaling pathway by virtual screening
文献类型：期刊论文
| 作者 | Zhang, Mingming1; Zhu, Weiliang2 ; Ding, Ning1; Zhang, Wei1; Li, Yingxia1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2013-04-01 |
| 卷号 | 23期号:7页码:2225-2229 |
| 关键词 | STAT3 signaling Small-molecule inhibitors Virtual screening Cell viability Antitumor activity |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2013.01.056 |
| 文献子类 | Article |
| 英文摘要 | Inhibition of the signal transducer and activator of transcription 3 (STAT3) signaling pathway has been considered a novel therapeutic strategy to treat human cancers that harbor aberrantly-active STAT3. In this study, a series of small molecules were identified as novel inhibitors of STAT3 signaling pathway through virtual screening. A tricyclic scaffold containing compound, 6, was identified as an inhibitor of IL-6/STAT3 signaling with an IC50 of 26.681 mu M. In addition, this compound inhibited Tyr705 phosphorylation of STAT3 and had no obvious effect on upstream tyrosine kinases. Thus, compound 6 is a potential lead structure and valuable for further drug development. (C) 2013 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ACCURATE DOCKING ; DESIGN ; GLIDE |
| 资助项目 | 11th Fudan University Graduates Innovation Project[00000000] ; National Natural Science Foundation of China[81072525] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000316642900063 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277673]  |
| 专题 | 药物发现与设计中心 |
| 通讯作者 | Li, Yingxia |
| 作者单位 | 1.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Mingming,Zhu, Weiliang,Ding, Ning,et al. Identification and characterization of small molecule inhibitors of signal transducer and activator of transcription 3 (STAT3) signaling pathway by virtual screening[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(7):2225-2229. |
| APA | Zhang, Mingming,Zhu, Weiliang,Ding, Ning,Zhang, Wei,&Li, Yingxia.(2013).Identification and characterization of small molecule inhibitors of signal transducer and activator of transcription 3 (STAT3) signaling pathway by virtual screening.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(7),2225-2229. |
| MLA | Zhang, Mingming,et al."Identification and characterization of small molecule inhibitors of signal transducer and activator of transcription 3 (STAT3) signaling pathway by virtual screening".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.7(2013):2225-2229. |
入库方式： OAI收割
来源：上海药物研究所
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