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 |
DOI | 10.1016/j.bmc.2016.06.035 |
收录类别 | SCI |
语种 | 英语 |
WOS记录号 | WOS:000380515700001 |
引用统计 | |
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 |
推荐引用方式 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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文件名称/大小 | 文献类型 | 版本类型 | 开放类型 | 使用许可 | ||
The design strategy (2312KB) | 期刊论文 | 出版稿 | 限制开放 | CC BY-NC-SA | 浏览 |
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