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ID: ALA2396625

Journal: Bioorg Med Chem Lett

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

Authors: Min G, Lee SK, Kim HN, Han YM, Lee RH, Jeong DG, Han DC, Kwon BM.

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.

CiteXplore: 23726031

DOI: 10.1016/j.bmcl.2013.04.092