Negative regulation of p120GAP GTPase promoting activity by p210bcr/abl: implication for RAS-dependent Philadelphia chromosome positive cell growth

J Exp Med. 1994 Jun 1;179(6):1855-65. doi: 10.1084/jem.179.6.1855.

Abstract

The p210bcr/abl tyrosine kinase appears to be responsible for initiating and maintaining the leukemic phenotype in chronic myelogenous leukemia (CML) patients. p21ras-p120GAP interactions play a central role in transducing mitogenic signals. Therefore, we investigated whether p21ras and p120GAP are regulated by p210bcr/abl, and whether this activation is functionally significant for CML cell proliferation. We report that transient expression of p210bcr/abl in fibroblast-like cells induces simultaneous activation of p21ras and inhibition of GTPase-promoting activity of p120GAP, and confirm these data showing that downregulation of p210bcr/abl expression in CML cells with bcr/abl antisense oligodeoxynucleotides induces both inhibition of p21ras activation and stimulation of GTPase-promoting activity of p120GAP. Tyrosine phosphorylation of two p120GAP-associated proteins, p190 and p62, which may affect p120GAP activity, also depends on p210bcr/abl tyrosine kinase expression. Direct dependence of these effects on the kinase activity is proven in experiments in which expression of c-MYB protein in fibroblast-like cells or downregulation of c-MYB expression resulting in analogous inhibition of CML cell proliferation does not result in the same changes. Use of specific antisense oligodeoxynucleotides to downregulate p21ras expression revealed a requirement for functional p21ras in the proliferation of Philadelphia chromosome-positive CML primary cells. Thus, the p210bcr/abl-dependent regulation of p120GAP activity is responsible, in part, for the maintenance of p21ras in the active GTP-bound form, a crucial requirement for CML cell proliferation.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Base Sequence
  • Cell Division / drug effects
  • Cell Division / physiology*
  • Cell Line
  • Chromosomes, Human, Pair 15
  • Chromosomes, Human, Pair 17
  • Chromosomes, Human, Pair 22
  • Chromosomes, Human, Pair 9
  • Fusion Proteins, bcr-abl / metabolism*
  • GTP Phosphohydrolases / metabolism*
  • GTPase-Activating Proteins
  • Gene Expression Regulation, Neoplastic / drug effects*
  • Homeostasis
  • Humans
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / genetics
  • Molecular Sequence Data
  • Oligonucleotides, Antisense / pharmacology*
  • Oncogenes / drug effects
  • Philadelphia Chromosome*
  • Proteins / metabolism*
  • Proto-Oncogene Proteins p21(ras) / metabolism*
  • Proto-Oncogenes / drug effects
  • Signal Transduction
  • Translocation, Genetic
  • Tumor Cells, Cultured
  • ras GTPase-Activating Proteins

Substances

  • GTPase-Activating Proteins
  • Oligonucleotides, Antisense
  • Proteins
  • ras GTPase-Activating Proteins
  • Fusion Proteins, bcr-abl
  • GTP Phosphohydrolases
  • HRAS protein, human
  • Proto-Oncogene Proteins p21(ras)