Phosphatase of regenerating liver-3 as a convergent therapeutic target for lymph node metastasis in esophageal squamous cell carcinoma

Int J Cancer. 2010 Aug 1;127(3):543-54. doi: 10.1002/ijc.25082.

Abstract

Phosphatase of regenerating liver-3 (PRL-3) is a molecule associated with metastasis in a diverse of cancers, which, however, remains largely unknown in esophageal squamous cell carcinoma (ESCC). We examined both the clinical significance of PRL-3 expression and its biological roles, and assessed possibilities as a therapeutic target in ESCC. PRL-3 expression was found in 78% (69 of 88) of the primary ESCC on immunohistochemistry; it was the strong independent predictor for lymph node metastasis (LNM) on a multivariate logistic regression model (p = 0.0014, relative risk =15.20). Additionally, gene amplification was found in 3 (7.9%) of the 38 primary tumors with PRL-3 overexpression by fluorescence in situ hybridization, but in none of the 19 tumors without it. PRL-3 small interfering RNA robustly repressed cell proliferation, anchorage-independent colony formation and invasion and augmented 5-FU-induced apoptosis in all the tested ESCC cell lines with PRL-3 overexpression, irrespective of its gene amplification status. PRL-3 inhibitor (1-4-bromo-2-benzylidene rhodanine) also suppressed such metastatic properties in the cell lines with PRL-3 overexpression, but not with its low expression. Inverse effects were observed by PRL-3 forced expression. Collectively, PRL-3 overexpression is a frequent event associated with LNM and plays a causative role in promoting cancer progression. Moreover, the expression status may be a landmark to select patients with benefit from PRL-3-targeted therapy. Thus, PRL-3 could be a convergent therapeutic target against ESCC with LNM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis
  • Blotting, Western
  • Carcinoma, Squamous Cell / drug therapy*
  • Carcinoma, Squamous Cell / pathology
  • Cell Cycle
  • Cell Line, Tumor
  • Cell Proliferation
  • Enzyme Inhibitors / pharmacology*
  • Esophageal Neoplasms / drug therapy*
  • Esophageal Neoplasms / pathology
  • Fluorescent Antibody Technique
  • Gene Expression Regulation, Enzymologic / drug effects
  • Humans
  • Immunohistochemistry
  • In Situ Hybridization, Fluorescence
  • Lymphatic Metastasis / physiopathology*
  • Middle Aged
  • Multivariate Analysis
  • Neoplasm Proteins / antagonists & inhibitors*
  • Neoplasm Proteins / genetics
  • Neoplasm Proteins / physiology
  • Polymerase Chain Reaction
  • Protein Tyrosine Phosphatases / antagonists & inhibitors*
  • Protein Tyrosine Phosphatases / genetics
  • Protein Tyrosine Phosphatases / physiology
  • RNA, Small Interfering
  • Rhodanine / analogs & derivatives*
  • Rhodanine / pharmacology

Substances

  • 1-(2-bromobenzyloxy)-4-bromo-2-benzylidene rhodanine
  • Enzyme Inhibitors
  • Neoplasm Proteins
  • RNA, Small Interfering
  • Rhodanine
  • PTP4A3 protein, human
  • Protein Tyrosine Phosphatases