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The design strategy of selective PTP1B inhibitors over TCPTP
Li, XiangQian; Wang, LiJun; Shi, DaYong1
2016-08-15
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY
卷号24期号:16页码:3343-3352
文章类型Review
摘要Protein tyrosine phosphatase 1B (PTP1B) has already been well studied as a highly validated therapeutic target for diabetes and obesity. However, the lack of selectivity limited further studies and clinical applications of PTP1B inhibitors, especially over T-cell protein tyrosine phosphatase (TCPTP). In this review, we enumerate the published specific inhibitors of PTP1B, discuss the structure-activity relationships by analysis of their X-ray structures or docking results, and summarize the characteristic of selectivity related residues and groups. Furthermore, the design strategy of selective PTP1B inhibitors over TCPTP is also proposed. We hope our work could provide an effective way to gain specific PTP1B inhibitors. (C) 2016 Elsevier Ltd. All rights reserved.
关键词Selectivity Ptp1b Inhibitor Tcptp Diabetes Design Strategy
DOI10.1016/j.bmc.2016.06.035
收录类别SCI
语种英语
WOS记录号WOS:000380515700001
引用统计
被引频次:12[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/337002/135858
专题海洋生物技术研发中心
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
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Li, XiangQian,Wang, LiJun,Shi, DaYong. The design strategy of selective PTP1B inhibitors over TCPTP[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2016,24(16):3343-3352.
APA Li, XiangQian,Wang, LiJun,&Shi, DaYong.(2016).The design strategy of selective PTP1B inhibitors over TCPTP.BIOORGANIC & MEDICINAL CHEMISTRY,24(16),3343-3352.
MLA Li, XiangQian,et al."The design strategy of selective PTP1B inhibitors over TCPTP".BIOORGANIC & MEDICINAL CHEMISTRY 24.16(2016):3343-3352.
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