LYN is a mediator of epithelial-mesenchymal transition and a target of dasatinib in breast cancer

Cancer Res. 2010 Mar 15;70(6):2296-306. doi: 10.1158/0008-5472.CAN-09-3141. Epub 2010 Mar 9.

Abstract

Epithelial-mesenchymal transition (EMT), a switch of polarized epithelial cells to a migratory, fibroblastoid phenotype, is considered a key process driving tumor cell invasiveness and metastasis. Using breast cancer cell lines as a model system, we sought to discover gene expression signatures of EMT with clinical and mechanistic relevance. A supervised comparison of epithelial and mesenchymal breast cancer lines defined a 200-gene EMT signature that was prognostic across multiple breast cancer cohorts. The immunostaining of LYN, a top-ranked EMT signature gene and Src-family tyrosine kinase, was associated with significantly shorter overall survival (P = 0.02) and correlated with the basal-like ("triple-negative") phenotype. In mesenchymal breast cancer lines, RNAi-mediated knockdown of LYN inhibited cell migration and invasion, but not proliferation. Dasatinib, a dual-specificity tyrosine kinase inhibitor, also blocked invasion (but not proliferation) at nanomolar concentrations that inhibit LYN kinase activity, suggesting that LYN is a likely target and that invasion is a relevant end point for dasatinib therapy. Our findings define a prognostically relevant EMT signature in breast cancer and identify LYN as a mediator of invasion and a possible new therapeutic target (and theranostic marker for dasatinib response), with particular relevance to clinically aggressive basal-like breast cancer.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Breast Neoplasms / enzymology*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / pathology*
  • Cell Line, Tumor
  • Dasatinib
  • Epithelial Cells / pathology
  • Female
  • Gene Expression Profiling
  • Humans
  • Mesoderm / pathology
  • Prognosis
  • Protein Kinase Inhibitors / pharmacology*
  • Pyrimidines / pharmacology*
  • Thiazoles / pharmacology*
  • src-Family Kinases / antagonists & inhibitors
  • src-Family Kinases / biosynthesis
  • src-Family Kinases / genetics*

Substances

  • Protein Kinase Inhibitors
  • Pyrimidines
  • Thiazoles
  • lyn protein-tyrosine kinase
  • src-Family Kinases
  • Dasatinib