Somatic mutations of ErbB4: selective loss-of-function phenotype affecting signal transduction pathways in cancer

J Biol Chem. 2009 Feb 27;284(9):5582-91. doi: 10.1074/jbc.M805438200. Epub 2008 Dec 19.

Abstract

Cancer drugs targeting ErbB receptors, such as epidermal growth factor receptor and ErbB2, are currently in clinical use. However, the role of ErbB4 as a potential cancer drug target has remained controversial. Recently, somatic mutations altering the coding region of ErbB4 were described in patients with breast, gastric, colorectal, or non-small cell lung cancer, but the functional significance of these mutations is unknown. Here we demonstrate that 2 of 10 of the cancer-associated mutations of ErbB4 lead to loss of ErbB4 kinase activity due to disruption of functionally important structural features. Interestingly, the kinase-dead ErbB4 mutants were as efficient as wild-type ErbB4 in forming a heterodimeric neuregulin receptor with ErbB2 and promoting phosphorylation of Erk1/2 and Akt in an ErbB2 kinase-dependent manner. However, the mutant ErbB4 receptors failed to phosphorylate STAT5 and suppressed differentiation of MDA-MB-468 mammary carcinoma cells. These findings suggest that the somatic ErbB4 mutations have functional consequences and lead to selective changes in ErbB4 signaling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • COS Cells
  • Cell Culture Techniques
  • Cell Differentiation
  • Cell Proliferation
  • Chlorocebus aethiops
  • ErbB Receptors / genetics*
  • ErbB Receptors / metabolism
  • Humans
  • Immunoprecipitation
  • Mitogen-Activated Protein Kinase 1 / metabolism*
  • Mitogen-Activated Protein Kinase 3 / metabolism*
  • Models, Molecular
  • Mutation / genetics*
  • Phenotype
  • Phosphorylation
  • Proto-Oncogene Proteins c-akt / metabolism*
  • Receptor, ErbB-2 / metabolism
  • Receptor, ErbB-4
  • STAT5 Transcription Factor / metabolism*
  • Signal Transduction*

Substances

  • STAT5 Transcription Factor
  • ERBB2 protein, human
  • ERBB4 protein, human
  • ErbB Receptors
  • Receptor, ErbB-2
  • Receptor, ErbB-4
  • Proto-Oncogene Proteins c-akt
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3