Targeting of the N-terminal coiled coil oligomerization interface of BCR interferes with the transformation potential of BCR-ABL and increases sensitivity to STI571

Blood. 2003 Oct 15;102(8):2985-93. doi: 10.1182/blood-2003-03-0811. Epub 2003 Jun 26.

Abstract

Translocations involving the abl locus on chromosome 9 fuses the tyrosine kinase c-ABL to proteins harboring oligomerization interfaces such as BCR or TEL, enabling these ABL-fusion proteins (X-ABL) to transform cells and to induce leukemia. The ABL kinase activity is blocked by the ABL kinase inhibitor STI571 which abrogates transformation by X-ABL. To investigate the role of oligomerization for the transformation potential of X-ABL and for the sensitivity to STI571, we constructed ABL chimeras with oligomerization interfaces of proteins involved in leukemia-associated translocations such as BCR, TEL, PML, and PLZF. We assessed the capacity of these chimeras to form high molecular weight (HMW) complexes as compared with p185(BCR-ABL). There was a direct relationship between the size of HMW complexes formed by these chimeras and their capacity to induce factor independence in Ba/F3 cells, whereas there was an inverse relationship between the size of the HMW complexes and the sensitivity to STI571. The targeting of the oligomerization interface of p185(BCR-ABL) by a peptide representing the coiled coil region of BCR reduced its potential to transform fibroblasts and increased sensitivity to STI571. Our results indicate that targeting of the oligomerization interfaces of the X-ABL enhances the effects of STI571 in the treatment of leukemia caused by X-ABL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Benzamides
  • Blotting, Western
  • COS Cells
  • Cell Line
  • Cell Line, Transformed
  • Cell Transformation, Neoplastic
  • DNA, Complementary / metabolism
  • Fibroblasts / metabolism
  • Fusion Proteins, bcr-abl / chemistry*
  • Imatinib Mesylate
  • Inhibitory Concentration 50
  • Leukemia / drug therapy
  • Mice
  • Microscopy, Fluorescence
  • Mutation
  • Oncogene Proteins / metabolism*
  • Phosphorylation
  • Piperazines / pharmacology*
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Tertiary
  • Protein-Tyrosine Kinases*
  • Proto-Oncogene Proteins c-bcr
  • Proto-Oncogene Proteins*
  • Pyrimidines / pharmacology*
  • Rats
  • Recombinant Fusion Proteins / metabolism
  • Retroviridae / genetics
  • Time Factors

Substances

  • Antineoplastic Agents
  • Benzamides
  • DNA, Complementary
  • Oncogene Proteins
  • Piperazines
  • Proto-Oncogene Proteins
  • Pyrimidines
  • Recombinant Fusion Proteins
  • Imatinib Mesylate
  • Protein-Tyrosine Kinases
  • Fusion Proteins, bcr-abl
  • Bcr protein, mouse
  • Proto-Oncogene Proteins c-bcr