Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors
文献类型：期刊论文
| 作者 | 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 |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2017-07-07 |
| 卷号 | 134页码:24-33 |
| 关键词 | PTP1B Bromophenol Saccharide Selectivity Permeability |
| 英文摘要 | 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. |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000401677500003 |
| 版本 | 出版稿 |
| 源URL | [http://ir.qdio.ac.cn/handle/337002/136870]  |
| 专题 | 海洋研究所_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 |
| 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. |
入库方式： OAI收割
来源：海洋研究所
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