Truncated, desensitization-defective neurokinin receptors mediate sustained MAP kinase activation, cell growth and transformation by a Ras-independent mechanism

EMBO J. 1996 Jul 1;15(13):3351-60.

Abstract

We have used the neurokinin NK-2 receptor as a model to examine how receptor desensitization affects cellular responses. The liganded receptor transiently activates phospholipase C (PLC) and is rapidly phosphorylated on Ser/Thr residues in its C-terminal domain. Mutant receptors lacking this domain mediate persistent activation of PLC. We now show that, in transfected Rat-1 cells, mutant receptor mediates ligand-induced DNA synthesis, morphological transformation and growth in soft agar, whereas wild-type (wt) receptor does not. Wt receptor causes only transient MAP kinase activation. In contrast, MAP kinase activation by mutant receptor is sustained for >4 h. Neither wt nor mutant receptor couples to Ras activation. Downregulation of protein kinase C (PKC) has little effect on MAP kinase activation, DNA synthesis and transformation. Mutant receptors also promote stronger protein tyrosine phosphorylation and stress fibre formation than does wt receptor. Thus, C-terminal truncation allows the NK-2 receptor to signal sustained MAP kinase activation, cell growth and transformation by a Ras- and PKC-independent mechanism. Our results reveal the importance of the C-terminal 'desensitization domain' in suppressing the oncogenic potential of a prototypic PLC-coupled receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ADP Ribose Transferases / metabolism
  • Animals
  • Botulinum Toxins*
  • Cell Division / genetics*
  • Cell Line
  • Cell Transformation, Neoplastic / genetics*
  • Enzyme Activation
  • Hydrolysis
  • Phenotype
  • Phosphatidylinositols / metabolism
  • Phosphorylation
  • Protein Kinases / metabolism*
  • Protein Serine-Threonine Kinases / metabolism
  • Proto-Oncogene Proteins / metabolism
  • Proto-Oncogene Proteins c-raf
  • Rats
  • Receptors, Neurokinin-2 / genetics
  • Receptors, Neurokinin-2 / metabolism*
  • Tyrosine / metabolism
  • ras Proteins / metabolism*

Substances

  • Phosphatidylinositols
  • Proto-Oncogene Proteins
  • Receptors, Neurokinin-2
  • Tyrosine
  • ADP Ribose Transferases
  • exoenzyme C3, Clostridium botulinum
  • Protein Kinases
  • Protein Serine-Threonine Kinases
  • Proto-Oncogene Proteins c-raf
  • Botulinum Toxins
  • ras Proteins