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Title 

Rhodanine-based PRL-3 inhibitors blocked the migration and invasion of metastatic cancer cells

 

로다닌 유도체의 암 전이 억제 효과

Authors 

Garam MinS K LeeH N KimYoung-Min HanR H LeeDae Gwin JeongDong Cho HanByoung-Mog Kwon

Publisher 

Elsevier

Issue Date 

2013

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 23, no. 13, pp. 3769-3774

Keywords 

InvasionMetastasisMigrationPRL-3Rhodanine

Abstract 

PRL-3, phosphatase of regenerating liver-3, plays a role in cancer progression through its involvement in invasion, migration, metastasis, and angiogenesis. We synthesized rhodanine derivatives, CG-707 and BR-1, which inhibited PRL-3 enzymatic activity with IC50 values of 0.8 μM and 1.1 μM, respectively. CG-707 and BR-1 strongly inhibited the migration and invasion of PRL-3 overexpressing colon cancer cells without exhibiting cytotoxicity. The specificity of the inhibitors on PRL-3 phosphatase activity was confirmed by the phosphorylation recovery of known PRL-3 substrates such as ezrin and cytokeratin 8. The compounds selectively inhibited PRL-3 in comparison with other phosphatases, and CG-707 regulated epithelial-to-mesenchymal transition (EMT) marker proteins. The results of the present study reveal that rhodanine is a specific PRL-3 inhibitor and a good lead molecule for obtaining a selective PRL-3 inhibitor.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2013.04.092

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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