Discovery of Bisindole as a Novel Scaffold for Protein Tyrosine Phosphatase 1B Inhibitors
文献类型：期刊论文
| 作者 | Jing, Changcheng1; Li, Ziyan1; Jia, Kaili1; Chen, Chen1; Liu, Xiao1; Wang, Beibei2; Hu, Wenhao; Li, Jia2 ; Zhu, Tong1; Dong, Suzhen1
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| 刊名 | ARCHIV DER PHARMAZIE
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| 出版日期 | 2017-01 |
| 卷号 | 350期号:1 |
| 关键词 | Inhibitor Mixed 3,3 '-bisindoles Molecular docking Protein tyrosine phosphatase 1B |
| ISSN号 | 0365-6233 |
| DOI | 10.1002/ardp.201600173 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) has been proposed to be an effective target for the treatment of both type II diabetes and obesity. However, no PTP1B inhibitor has come into clinic application. Herein, we report mixed 3,3'-bisindoles as novel PTP1B inhibitors with low micromole-ranged inhibitory activity. The best active compound 9f inhibited PTP1B activity with an IC50 of 2.79 mu M. Meanwhile, it had low cytotoxicity and enhanced glucose uptake in vitro. Further studies demonstrated that some of these active compounds had a specific selectivity over other PTPs. Computational analysis further showed the binding mode of compound 9f with the active pocket of PTP1B. Our studies provide a novel scaffold for further development of more promising PTP1B inhibitors and potential drugs for type II diabetes and obesity. |
| WOS关键词 | INSULIN SENSITIVITY ; GLUCOSE-UPTAKE ; RESISTANCE ; PTP1B ; MICE ; OBESITY ; ACID ; GENE |
| 资助项目 | National Natural Science Foundation of China[21125209] ; National Natural Science Foundation of China[21403068] ; Natural Science Foundation of Shanghai[16ZR141050] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000396362200008 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275725]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
| 通讯作者 | Zhu, Tong; Dong, Suzhen |
| 作者单位 | 1.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, 3663 Zhongshan Rd N, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Chinese Natl Ctr Drug Screening, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jing, Changcheng,Li, Ziyan,Jia, Kaili,et al. Discovery of Bisindole as a Novel Scaffold for Protein Tyrosine Phosphatase 1B Inhibitors[J]. ARCHIV DER PHARMAZIE,2017,350(1). |
| APA | Jing, Changcheng.,Li, Ziyan.,Jia, Kaili.,Chen, Chen.,Liu, Xiao.,...&Dong, Suzhen.(2017).Discovery of Bisindole as a Novel Scaffold for Protein Tyrosine Phosphatase 1B Inhibitors.ARCHIV DER PHARMAZIE,350(1). |
| MLA | Jing, Changcheng,et al."Discovery of Bisindole as a Novel Scaffold for Protein Tyrosine Phosphatase 1B Inhibitors".ARCHIV DER PHARMAZIE 350.1(2017). |
入库方式： OAI收割
来源：上海药物研究所
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