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Bioorg Med Chem Lett. 2012 Jan 1;22(1):323-6. doi: 10.1016/j.bmcl.2011.11.008. Epub 2011 Nov 9.

Emodin inhibits migration and invasion of DLD-1 (PRL-3) cells via inhibition of PRL-3 phosphatase activity.

Author information

1
Laboratory of Chemical Genomics and Biology, Korea Research Institute of Bioscience and Biotechnology, 1125 Gwahakro, Yoosunggu, Daejeon 305-600, Republic of Korea.

Abstract

Anthraquinones have been reported as phosphatase inhibitors. Therefore, anthraquinone derivatives were screened to identify a potent phosphatase inhibitor against the phosphatase of regenerating liver-3 (PRL-3). Emodin strongly inhibited phosphatase activity of PRL-3 with IC(50) values of 3.5μM and blocked PRL-3-induced tumor cell migration and invasion in a dose-dependent manner. Emodin rescued the phosphorylation of ezrin, which is a known PRL-3 substrate. The results of this study reveal that emodin is a PRL-3 inhibitor and a good lead molecule for obtaining a selective PRL-3 inhibitor.

PMID:
22137788
DOI:
10.1016/j.bmcl.2011.11.008
[Indexed for MEDLINE]

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