| Kinetics of Phosphatase of Regenerating Liver-3 （PRL-3） Inhibition by Small-molecular Inhibitors |
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| 作者姓名： | SHEN Xing-gui SUN Li-wen JIAO Ming LI Zhao-fa ZHAO Zhi-zhuang LI Qing-shan FU Xue-qi ** and HUANG Zhong-xiu . Edmond H. Fischer Signal Transduction Laboratory College of Life Sciences Jilin University Changchun P. R. China . Qianwei Campus Clinical Hospital of Jilin University Changchun P. R. China |
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| 作者单位： | SHEN Xing-gui 1，SUN Li-wen 1，JIAO Ming 1，LI Zhao-fa 1，ZHAO Zhi-zhuang 1，LI Qing-shan 1，FU Xue-qi 1** and HUANG Zhong-xiu 21. Edmond H. Fischer Signal Transduction Laboratory，College of Life Sciences，Jilin University，Changchun 130021，P. R. China;2. Qianwei Campus Clinical Hospital of Jilin University，Changchun 130021，P. R. China |
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| 基金项目： | Supported by the National Natural Science Foundation of China（ No. 30470391 ）. |
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| 摘 要： | Introduction Proteintyrosinephosphatases(PTPs)playakey roleinsignaltransductionpathways,whichregulatethe growth,differentiationandmalignanttransformationof cells1].PhosphataseofRegeneratingLiver3(PRL3)belongstoarecentlydiscoveredfamilyofproteinphos phata…
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| 关 键 词： | 磷酸酯酶 PRL-3 DiFMUP 动力学 抑制剂 结肠直肠癌 蛋白质 |
| 文章编号： | 1005-9040（2006）-02-221-04 |
| 收稿时间： | 2005-12-20 |
Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors |
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| SHEN Xing-gui ,SUN Li-wen ,JIAO Ming ,LI Zhao-fa ,ZHAO Zhi-zhuang ,LI Qing-shan ,FU Xue-qi ** and HUANG Zhong-xiu . Edmond H. Fischer Signal Transduction Laboratory,College of Life Sciences,Jilin University,Changchun ,P. R. China,. Qianwei Campus Clinical Hospital of Jilin University,Changchun ,P. R. China.Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors[J].Chemical Research in Chinese University,2006,22(2):221-224. |
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| Authors: | Xing-gui SHEN Li-wen SUN Ming JIAO Zhao-fa LI Zhi-zhuang ZHAO Qing-shan LI Xue-qi FU Zhong-xiu HUANG |
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| Institution: | aEdmond H. Fischer Signal Transduction Laboratory, College of Life Sciences, Jilin University, Changchun 130021, P. R. China;bQianwei Campus Clinical Hospital of Jilin University, Changchun 130021, P. R. China |
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| Abstract: | Phosphatase of Regenerating Liver-3 (PRL-3) is a newly identified colorectal cancer metastasis-related protein,which isa 22 kDa non-classical protein tyrosine phosphatase with a C-terminal prenylation motif. In this study, the inhibition kinetics of protein tyrosine phosphatases (PTPs) by a fluorescent substrate, 6,8-difluoro-4-methylumbelliferyl phosphate (DiFMUP) was evaluated. PRL-3 exhibits classical Michaelis-Menten kinetics with a vmax value of the inhibitor magnolol can cause Km to increase, but does not alter the vmax value, which suggests the competitive inhibition of PRL-3. At the same time, it was found that DiFMUP is a more sensitive substrate for PRL-3 than para-nitrophenyl phosphate(pNPP) that is more frequently used at present. Furthermore, the method of screening for PTPs by the use of DiFMUP was developed, which studied the acceptance of DiFMUP by other PTPs. |
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| Keywords: | PRL-3 DiFMUP Kinetics Inhibitor |
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