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The design strategy of selective PTP1B inhibitors over TCPTP
Li, XiangQian; Wang, LiJun; Shi, DaYong1
2016-08-15
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY
Volume24Issue:16Pages:3343-3352
SubtypeReview
AbstractProtein 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.
KeywordSelectivity Ptp1b Inhibitor Tcptp Diabetes Design Strategy
DOI10.1016/j.bmc.2016.06.035
Indexed BySCI
Language英语
WOS IDWOS:000380515700001
Citation statistics
Cited Times:18[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Version出版稿
Identifierhttp://ir.qdio.ac.cn/handle/337002/135858
Collection海洋生物技术研发中心
Affiliation1.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
Recommended Citation
GB/T 7714
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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