title: Emodin inhibits migration and invasion of DLD-1 (PRL-3) cells via inhibition of PRL-3 phosphatase activity.
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.
authors.affiliation: Laboratory of Chemical Genomics and Biology, Korea Research Institute of Bioscience and Biotechnology, 1125 Gwahakro, Yoosunggu, Daejeon 305-600, Republic of Korea.
authors.forename: Young-Min
authors.initials: YM
authors.lastname: Han
authors.forename: Su-Kyung
authors.initials: SK
authors.lastname: Lee
authors.forename: Dae Gwin
authors.initials: DG
authors.lastname: Jeong
authors.forename: Seong Eon
authors.initials: SE
authors.lastname: Ryu
authors.forename: Dong Cho
authors.initials: DC
authors.lastname: Han
authors.forename: Dae Keun
authors.initials: DK
authors.lastname: Kim
authors.forename: Byoung-Mog
authors.initials: BM
authors.lastname: Kwon
mesh_terms: D000880:Anthraquinones / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D045744:Cell Line, Tumor; D002465:Cell Movement; D003094:Collagen / Q000737:chemistry; D003110:Colonic Neoplasms / Q000473:pathology; D004305:Dose-Response Relationship, Drug; D004338:Drug Combinations; D015195:Drug Design; D004642:Emodin / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D007797:Laminin / Q000737:chemistry; D008956:Models, Chemical; D009361:Neoplasm Invasiveness; D009363:Neoplasm Proteins / Q000378:metabolism*; D009369:Neoplasms / Q000473:pathology; D010766:Phosphorylation; D017027:Protein Tyrosine Phosphatases / Q000378:metabolism*; D011509:Proteoglycans / Q000737:chemistry
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; D004338:Drug Combinations; D007797:Laminin; D009363:Neoplasm Proteins; D011509:Proteoglycans; C059485:matrigel; D003094:Collagen; C484730:PTP4A3 protein, human; D017027:Protein Tyrosine Phosphatases; D004642:Emodin