Protein tyrosine phosphatases as drug targets: strategies and challenges of inhibitor development

被引：217

作者：

Barr, Alastair J. ^{[1
]}

机构：

[1] Univ Oxford, Struct Genom Consortium, Oxford OX3 7DQ, England

来源：

FUTURE MEDICINAL CHEMISTRY | 2010年 / 2卷 / 10期

关键词：

1B INHIBITORS; INSULIN SENSITIVITY; THERAPEUTIC TARGET; CRYSTAL-STRUCTURE; BINDING-SITE; PTP1B; DISCOVERY; POTENT; SHP2; IDENTIFICATION;

D O I：

10.4155/FMC.10.241

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several 'classical' protein tyrosine phosphatases are attractive therapeutic targets, including PTPIB for obesity and Type II diabetes; SHP2 for cancer and Lyp for rheumatoid arthritis. Progress has been made in identifying a broad range of chemically distinct inhibitors; however, developing selective and cell-permeable clinically useful compounds has proved challenging. Here the ongoing challenges and recent significant advances in the field are reviewed. Key novel compounds are highlighted and a perspective on the future of phosphatase inhibitor development is presented.

引用

页码：1563 / 1576

页数：14

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