Viewing serine/threonine protein phosphatases through the eyes of drug designers.
Viewing serine/threonine protein phosphatases through the eyes of drug designers.
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从药物设计者的角度看丝氨酸/苏氨酸蛋白磷酸酶。
DOI：
10.1111/febs.12481
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发表时间：
2013-10
期刊：
影响因子：
--
通讯作者：
Zhang Y
中科院分区：
文献类型：
--
作者：
Zhang M;Yogesha SD;Mayfield JE;Gill GN;Zhang Y
Protein phosphatases, as the counterpart to protein kinases, are essential for homeostatic balance of cell signaling. Small chemical compounds that modulate the specific activity of phosphatases can be powerful tools to elucidate the biological functions of these enzymes. More importantly, many phosphatases are central players in the development of pathological pathways where inactivation can reverse or delay the onset of human diseases. Therefore, potent inhibitors for such phosphatases can be of great therapeutic benefit. In contrast to the seemingly identical enzymatic mechanism and structural characterization of eukaryotic protein kinases, protein phosphatases evolved from diverse ancestors, resulting in different domain architectures, reaction mechanisms and active site properties. In this review, we will discuss for each family of serine/threonine protein phosphatases, their involvement in biological process and corresponding strategies for small chemical intervention. Recent advances in modern drug discovery technologies have markedly facilitated the identification of selective inhibitors for some members of the phosphatase family. Furthermore, the rapid growth in knowledge about structure-activity relationships related to possible new drug targets has aided the discovery of natural product inhibitors for phosphatase family. This review summarizes the current state of investigation of the small molecules that regulate the function of serine/threonine phosphatases, the challenges presented and also strategies to overcome these obstacles.
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影响因子：
3.7
作者：
Ammosova T;Platonov M;Yedavalli VR;Obukhov Y;Gordeuk VR;Jeang KT;Kovalskyy D;Nekhai S
通讯作者：
Nekhai S
影响因子：
50.3
作者：
Chen M;Pratt CP;Zeeman ME;Schultz N;Taylor BS;O'Neill A;Castillo-Martin M;Nowak DG;Naguib A;Grace DM;Murn J;Navin N;Atwal GS;Sander C;Gerald WL;Cordon-Cardo C;Newton AC;Carver BS;Trotman LC
通讯作者：
Trotman LC
影响因子：
13.8
作者：
COHEN, P
通讯作者：
COHEN, P
影响因子：
13.8
作者：
Bollen, Mathieu;Peti, Wolfgang;Ragusa, Michael J.;Beullens, Monique
通讯作者：
Beullens, Monique
DOI：
10.1073/pnas.94.26.14300
发表时间：
1997-12-23
影响因子：
11.1
作者：
Archambault, J;Chambers, RS;Greenblatt, J
通讯作者：
Greenblatt, J