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Design, synthesis and biological evaluation of uncharged catechol derivatives as selective inhibitors of PTP1B
Li, Xiang-Qian1,2; Xu, Qi1,2,3; Luo, Jiao1,2,3; Wang, Li-Jun1,2; Jiang, Bo1,2; Zhang, Ren-Shuai1,2; Shi, Da-Yong1,2,3
2017-08-18
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷号136页码:348-359
文章类型Article
摘要Protein tyrosine phosphatases 1B (PTP1B) is a promising and validated therapeutic target to effectively treat T2DM and obesity. However, the development of charged PTP1B inhibitors was restricted due to their low cell permeability and poor bioavailability. Based on active natural products, two series of uncharged catechol derivatives were identified as PTP1B inhibitors by targeting a secondary aryl phosphate-binding site as well as the catalytic site. The most potent inhibitor 22 showed an IC50 of 0.487 mu M against PTP1B and strong selectivity (27-fold) over TCPTP. Kinetic studies were also performed that 22 act as a competitive PTP1B inhibitor. The treatment of C2C12 myotubes with 22 markedly increased the phosphorylation levels of IR beta, Akt and IRS1 phosphorylation. The similarity of its action profiling with that produced by insulin suggested its potential as a new non-insulin-dependent drug candidate. (C) 2017 Elsevier Masson SAS. All rights reserved.
关键词Type 2 Diabetes Ptp1b Inhibition Selectivity Competitive Cellular Activity
DOI10.1016/j.ejmech.2017.05.007
收录类别SCI
语种英语
WOS记录号WOS:000403993500029
引用统计
被引频次:3[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/337002/137139
专题实验海洋生物学重点实验室
作者单位1.Chinese Acad Sci, Inst Oceanol, Key Lab Expt Marine Biol, 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
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Li, Xiang-Qian,Xu, Qi,Luo, Jiao,et al. Design, synthesis and biological evaluation of uncharged catechol derivatives as selective inhibitors of PTP1B[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2017,136:348-359.
APA Li, Xiang-Qian.,Xu, Qi.,Luo, Jiao.,Wang, Li-Jun.,Jiang, Bo.,...&Shi, Da-Yong.(2017).Design, synthesis and biological evaluation of uncharged catechol derivatives as selective inhibitors of PTP1B.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,136,348-359.
MLA Li, Xiang-Qian,et al."Design, synthesis and biological evaluation of uncharged catechol derivatives as selective inhibitors of PTP1B".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 136(2017):348-359.
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