Geldanamycin abrogates ErbB2 association with proteasome-resistant beta-catenin in melanoma cells, increases beta-catenin-E-cadherin association, and decreases beta-catenin-sensitive transcription

Cancer Res. 2001 Feb 15;61(4):1671-7.

Abstract

Beta-catenin undergoes both serine and tyrosine phosphorylation. Serine phosphorylation in the amino terminus targets beta-catenin for proteasome degradation, whereas tyrosine phosphorylation in the COOH terminus influences interaction with E-cadherin. We examined the tyrosine phosphorylation status of beta-catenin in melanoma cells expressing proteasome-resistant beta-catenin, as well as the effects that perturbation of beta-catenin tyrosine phosphorylation had on its association with E-cadherin and on its transcriptional activity. Beta-catenin is tyrosine phosphorylated in three melanoma cell lines and associates with both the ErbB2 receptor tyrosine kinase and the LAR receptor tyrosine phosphatase. Geldanamycin, a drug which destabilizes ErbB2, caused rapid cellular depletion of the kinase and loss of its association with beta-catenin without perturbing either LAR or beta-catenin levels or LAR/beta-catenin association. Geldanamycin also stimulated tyrosine dephosphorylation of beta-catenin and increased beta-catenin/E-cadherin association, resulting in substantially decreased cell motility. Geldanamycin also decreased the nuclear beta-catenin level and inhibited beta-catenin-driven transcription, as assessed using two different beta-catenin-sensitive reporters and the endogenous cyclin D1 gene. These findings were confirmed by transient transfection of two beta-catenin point mutants, Tyr-654Phe and Tyr-654Glu, which, respectively, mimic the dephosphorylated and phosphorylated states of Tyr-654, a tyrosine residue contained within the beta-catenin-ErbB2-binding domain. These data demonstrate that the functional activity of proteasome-resistant beta-catenin is regulated further by geldanamycin-sensitive tyrosine phosphorylation in melanoma cells.

MeSH terms

  • Antibiotics, Antineoplastic / pharmacology*
  • Benzoquinones
  • Cadherins / metabolism*
  • Cell Movement / drug effects
  • Cysteine Endopeptidases / drug effects
  • Cysteine Endopeptidases / metabolism*
  • Cysteine Proteinase Inhibitors / pharmacology
  • Cytoskeletal Proteins / genetics
  • Cytoskeletal Proteins / metabolism*
  • Humans
  • Lactams, Macrocyclic
  • Melanoma / drug therapy
  • Melanoma / genetics
  • Melanoma / metabolism*
  • Melanoma / pathology
  • Multienzyme Complexes / drug effects
  • Multienzyme Complexes / metabolism*
  • Nerve Tissue Proteins*
  • Phosphorylation
  • Point Mutation
  • Proteasome Endopeptidase Complex
  • Protein Tyrosine Phosphatases / metabolism
  • Quinones / pharmacology*
  • Receptor, ErbB-2 / metabolism*
  • Receptor-Like Protein Tyrosine Phosphatases, Class 2
  • Receptor-Like Protein Tyrosine Phosphatases, Class 4
  • Receptors, Cell Surface / metabolism
  • Trans-Activators*
  • Transcription, Genetic / drug effects
  • Transcriptional Activation
  • Transfection
  • Tumor Cells, Cultured
  • Tyrosine / metabolism
  • beta Catenin

Substances

  • Antibiotics, Antineoplastic
  • Benzoquinones
  • CTNNB1 protein, human
  • Cadherins
  • Cysteine Proteinase Inhibitors
  • Cytoskeletal Proteins
  • Lactams, Macrocyclic
  • Multienzyme Complexes
  • Nerve Tissue Proteins
  • Quinones
  • Receptors, Cell Surface
  • Trans-Activators
  • beta Catenin
  • Tyrosine
  • Receptor, ErbB-2
  • PTPRA protein, human
  • PTPRF protein, human
  • Protein Tyrosine Phosphatases
  • Receptor-Like Protein Tyrosine Phosphatases, Class 2
  • Receptor-Like Protein Tyrosine Phosphatases, Class 4
  • Cysteine Endopeptidases
  • Proteasome Endopeptidase Complex
  • geldanamycin