| Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors | |
| Zhang, Renshuai1,2; Yu, Rilei4; Xu, Qi1,2; Li, Xiangqian1,2; Luo, Jiao1,2; Jiang, Bo1,2; Wang, Lijun1,2; Guo, Shuju1,2; Wu, Ning1,2; Shi, Dayong1,2,3 | |
| 2017-07-07 | |
| 发表期刊 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 卷号 | 134页码:24-33 |
| 文章类型 | Article |
| 摘要 | Protein tyrosine phosphatase 1B (PTP1B) is a key negative regulator of insulin signaling pathway. Inhibition of PTP1B is expected to improve insulin action. Appropriate selectivity and permeability are the gold standard for excellent PTP1B inhibitors. In this work, molecular hybridization-based screening identified a selective competitive PTP1B inhibitor. Compound 10a has IC50 values of 199 nM against PTP1B, and shows 32-fold selectivity for PTP1B over the closely related phosphatase TCPTP). Molecule docking and molecular dynamics studies reveal the reason of selectivity for PTP1B over TCPTP. Moreover, the cell permeability and cellular activity of compound 10a are demonstrated respectively. (C) 2017 Elsevier Masson SAS. All rights reserved. |
| 关键词 | Ptp1b Bromophenol Saccharide Selectivity Permeability |
| DOI | 10.1016/j.ejmech.2017.04.004 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000401677500003 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 版本 | 出版稿 |
| 条目标识符 | http://ir.qdio.ac.cn/handle/337002/136870 |
| 专题 | 海洋生物技术研发中心 |
| 作者单位 | 1.Chinese Acad Sci, Key Lab Expt Marine Biol, Inst Oceanol, Qingdao, Peoples R China 2.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao, Peoples R China 3.Univ Chinese Acad Sci, Beijing, Peoples R China 4.Ocean Univ China, Key Lab Marine Drugs, Minist Educ China, Sch Med & Pharm, Qingdao 266003, Peoples R China |
| 第一作者单位 | 中国科学院海洋研究所 |
| 推荐引用方式 GB/T 7714 | Zhang, Renshuai,Yu, Rilei,Xu, Qi,et al. Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2017,134:24-33. |
| APA | Zhang, Renshuai.,Yu, Rilei.,Xu, Qi.,Li, Xiangqian.,Luo, Jiao.,...&Shi, Dayong.(2017).Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,134,24-33. |
| MLA | Zhang, Renshuai,et al."Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 134(2017):24-33. |
| 条目包含的文件 | ||||||
| 文件名称/大小 | 文献类型 | 版本类型 | 开放类型 | 使用许可 | ||
| Discovery and evalua（3126KB） | 期刊论文 | 出版稿 | 限制开放 | CC BY-NC-SA | 浏览 | |
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