2. Academic Validation
  3. Rhodanine-based PRL-3 inhibitors blocked the migration and invasion of metastatic cancer cells

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

  • Bioorg Med Chem Lett. 2013 Jul 1;23(13):3769-74. doi: 10.1016/j.bmcl.2013.04.092.
Garam Min 1,  Su-Kyung Lee,  Hye-Nan Kim,  Young-Min Han,  Rhan-Hee Lee,  Dae Gwin Jeong,  Dong Cho Han,  Byoung-Mog Kwon
Affiliations

Affiliation

  • 1 Laboratory of Chemical Genomics and Biology, Korea Research Institute of Bioscience and Biotechnology, University of Science and Technology, 125 Gwahakro, Yoosunggu, Daejeon 305-600, Republic of Korea.
PMID: 23726031 DOI: 10.1016/j.bmcl.2013.04.092
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.

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