Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors

高等学校化学研究 ›› 2006, Vol. 22 ›› Issue (2): 221-224.

Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors

SHEN Xing-gui¹, SUN Li-wen¹, JIAO Ming¹, LI Zhao-fa¹, ZHAO Zhi-zhuang¹, LI Qing-shan¹, FU Xue-qi¹, HUANG Zhong-xiu²

1. 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

收稿日期:2005-12-20 出版日期:2006-04-24 发布日期:2011-08-06
基金资助:
Supported by the National Natural Science Foundation of China(No.30470391).

Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors

SHEN Xing-gui¹, SUN Li-wen¹, JIAO Ming¹, LI Zhao-fa¹, ZHAO Zhi-zhuang¹, LI Qing-shan¹, FU Xue-qi¹, HUANG Zhong-xiu²

1. 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

Received:2005-12-20 Online:2006-04-24 Published:2011-08-06
Supported by:
Supported by the National Natural Science Foundation of China(No.30470391).

摘要/Abstract

摘要： 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 v_max value of 11.3 -μmol· L^-1 · m in^-1.Analysis o f PRL-3 by aM ichae lis-M enten plot and a doub le-rec iprocal plot ind ica ted that the inhibitor magnolol can cause K_m to increase, but does not alter the v_max 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.

关键词: PRL-3, DiFMUP, Kinetics, Inhibitor

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 v_max value of 11.3 -μmol· L^-1 · m in^-1.Analysis o f PRL-3 by aM ichae lis-M enten plot and a doub le-rec iprocal plot ind ica ted that the inhibitor magnolol can cause K_m to increase, but does not alter the v_max 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.

Key words: PRL-3, DiFMUP, Kinetics, Inhibitor

SHEN Xing-gui, SUN Li-wen, JIAO Ming, LI Zhao-fa, ZHAO Zhi-zhuang, LI Qing-shan, FU Xue-qi, HUANG Zhong-xiu. Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors[J]. 高等学校化学研究, 2006, 22(2): 221-224.

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Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors

Kinetics of Phosphatase of Regenerating Liver-3 (PRL-3) Inhibition by Small-molecular Inhibitors

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