Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.323-326
2012
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Details
- Autor(en) / Beteiligte
- Titel
- Emodin inhibits migration and invasion of DLD-1 (PRL-3) cells via inhibition of PRL-3 phosphatase activity
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.323-326
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2012
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Emodin inhibited PRL-3 phosphatase activity and then blocked migration and invasion of DLD-1 (PRL-3) cells. And emodin rescued phosphorylation of ezrin in DLD (PRL-3) cells. 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 IC50 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2011.11.008Titel-ID: cdi_proquest_miscellaneous_918064424
- Format
- –
- Schlagworte
- Anthraquinones - pharmacology, Antineoplastic Agents - pharmacology, Biological and medical sciences, Cell Line, Tumor, Cell Movement, Collagen - chemistry, Colonic Neoplasms - pathology, Dose-Response Relationship, Drug, Drug Combinations, Drug Design, Emodin, Emodin - pharmacology, Humans, Inhibitory Concentration 50, Invasion, Laminin - chemistry, Medical sciences, Metastasis, Migration, Models, Chemical, Neoplasm Invasiveness, Neoplasm Proteins - metabolism, Neoplasms - pathology, Pharmacology. Drug treatments, Phosphorylation, PRL-3, Protein Tyrosine Phosphatases - metabolism, Proteoglycans - chemistry