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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
DOI10.1016/j.ejmech.2017.04.004
收录类别SCI
语种英语
WOS记录号WOS:000401677500003
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被引频次:4[WOS]   [WOS记录]     [WOS相关记录]
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
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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.
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