Receptor-type protein-tyrosine phosphatase-kappa regulates epidermal growth factor receptor function

J Biol Chem. 2005 Dec 30;280(52):42694-700. doi: 10.1074/jbc.M507722200. Epub 2005 Oct 31.

Abstract

Epidermal growth factor receptor (EGFR), the prototypic receptor protein tyrosine kinase, is a major regulator of growth and survival for many epithelial cell types. We report here that receptor-type protein-tyrosine phosphatase-kappa (RPTP-kappa) dephosphorylates EGFR and thereby regulates its function in human keratinocytes. Protein-tyrosine phosphatase (PTP) inhibitors induced EGFR tyrosine phosphorylation in intact primary human keratinocytes and cell-free membrane preparations. Five highly expressed RPTPs (RPTP-beta, delta, kappa, mu, and xi) were functionally analyzed in a Chinese hamster ovary (CHO) cell-based expression system. Full-length human EGFR expressed in CHO cells, which lack endogenous EGFR, displayed high basal (i.e. in the absence of ligand) tyrosine phosphorylation. Co-expression of RPTP-kappa, but not other RPTPs, specifically reduced basal EGFR tyrosine phosphorylation. RPTP-kappa also reduced epidermal growth factor-dependent EGFR tyrosine phosphorylation in CHO cells. Purified RPTP-kappa preferentially dephosphorylated EGFR tyrosines 1068 and 1173 in vitro. Overexpression of wild-type or catalytically inactive RPTP-kappa reduced or enhanced, respectively, basal and EGF-induced EGFR tyrosine phosphorylation in human keratinocytes. Furthermore, siRNA-mediated knockdown of RPTP-kappa increased basal and EGF-stimulated EGFR tyrosine phosphorylation and augmented downstream Erk activation in human keratinocytes. RPTP-kappa levels increased in keratinocytes as cells reached confluency, and overexpression of RPTP-kappa in subconfluent keratinocytes reduced keratinocyte proliferation. Taken together, the above data indicate that RPTP-kappa is a key regulator of EGFR tyrosine phosphorylation and function in human keratinocytes.

MeSH terms

  • Animals
  • Blotting, Western
  • CHO Cells
  • Cell Membrane / metabolism
  • Cell Proliferation
  • Cricetinae
  • Enzyme Activation
  • Epithelial Cells / cytology
  • Epithelial Cells / enzymology
  • ErbB Receptors / metabolism*
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Gene Expression Regulation, Enzymologic*
  • Genetic Vectors
  • Glutathione Transferase / metabolism
  • Humans
  • Keratinocytes / cytology
  • Keratinocytes / enzymology
  • Keratinocytes / metabolism
  • Mutation
  • Phosphorylation
  • Protein Tyrosine Phosphatases / metabolism
  • Protein Tyrosine Phosphatases / physiology*
  • RNA, Small Interfering / metabolism
  • Receptor-Like Protein Tyrosine Phosphatases, Class 2
  • Recombinant Fusion Proteins / metabolism
  • Transfection
  • Tyrosine / chemistry

Substances

  • RNA, Small Interfering
  • Recombinant Fusion Proteins
  • Tyrosine
  • Glutathione Transferase
  • ErbB Receptors
  • Extracellular Signal-Regulated MAP Kinases
  • PTPRK protein, human
  • Protein Tyrosine Phosphatases
  • Receptor-Like Protein Tyrosine Phosphatases, Class 2