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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
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume134Pages:24-33
SubtypeArticle
AbstractProtein 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.
KeywordPtp1b Bromophenol Saccharide Selectivity Permeability
DOI10.1016/j.ejmech.2017.04.004
Indexed BySCI
Language英语
WOS IDWOS:000401677500003
Citation statistics
Document Type期刊论文
Version出版稿
Identifierhttp://ir.qdio.ac.cn/handle/337002/136870
Collection海洋生物技术研发中心
Affiliation1.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
First Author Affilication中国科学院海洋研究所
Recommended Citation
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.
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