Targeting Protein Serine/Threonine Phosphatases for Drug Development

被引:138
作者
McConnell, Jamie L. [1 ]
Wadzinski, Brian E. [1 ]
机构
[1] Vanderbilt Univ, Dept Pharmacol, Med Ctr, Sch Med, Nashville, TN 37232 USA
基金
美国国家卫生研究院;
关键词
NF-KAPPA-B; SPHINGOSINE 1-PHOSPHATE RECEPTORS; 2A SUBUNIT INTERACTION; STRUCTURE-BASED DESIGN; TUMOR-SUPPRESSOR PP2A; MAP KINASE PATHWAY; SMALL-T-ANTIGEN; ANTICANCER ACTIVITY; CATALYTIC SUBUNIT; NORCANTHARIDIN ANALOGS;
D O I
10.1124/mol.108.053140
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
With the recent clinical success of drugs targeting protein kinase activity, drug discovery efforts are focusing on the role of reversible protein phosphorylation in disease states. The activity of protein phosphatases, enzymes that oppose protein kinases, can also be manipulated to alter cellular signaling for therapeutic benefits. In this review, we present protein serine/threonine phosphatases as viable therapeutic targets, discussing past successes, current challenges, and future strategies for modulating phosphatase activity.
引用
收藏
页码:1249 / 1261
页数:13
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