Phosphorylation of the ATP-binding loop directs oncogenicity of drug-resistant BCR-ABL mutants

Proc Natl Acad Sci U S A. 2006 Dec 19;103(51):19466-71. doi: 10.1073/pnas.0609239103. Epub 2006 Dec 12.

Abstract

The success of targeting kinases in cancer with small molecule inhibitors has been tempered by the emergence of drug-resistant kinase domain mutations. In patients with chronic myeloid leukemia treated with ABL inhibitors, BCR-ABL kinase domain mutations are the principal mechanism of relapse. Certain mutations are occasionally detected before treatment, suggesting increased fitness relative to wild-type p210 BCR-ABL. We evaluated the oncogenicity of eight kinase inhibitor-resistant BCR-ABL mutants and found a spectrum of potencies greater or less than p210. Although most fitness alterations correlate with changes in kinase activity, this is not the case with the T315I BCR-ABL mutation that confers clinical resistance to all currently approved ABL kinase inhibitors. Through global phosphoproteome analysis, we identified a unique phosphosubstrate signature associated with each drug-resistant allele, including a shift in phosphorylation of two tyrosines (Tyr253 and Tyr257) in the ATP binding loop (P-loop) of BCR-ABL when Thr315 is Ile or Ala. Mutational analysis of these tyrosines in the context of Thr315 mutations demonstrates that the identity of the gatekeeper residue impacts oncogenicity by altered P-loop phosphorylation. Therefore, mutations that confer clinical resistance to kinase inhibitors can substantially alter kinase function and confer novel biological properties that may impact disease progression.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Amino Acid Sequence
  • Animals
  • Cell Line
  • DNA Mutational Analysis
  • Drug Resistance, Neoplasm / genetics*
  • Fusion Proteins, bcr-abl / genetics*
  • Fusion Proteins, bcr-abl / metabolism*
  • Mass Spectrometry
  • Mice
  • Molecular Sequence Data
  • Mutation, Missense / genetics
  • Phosphorylation
  • Protein Binding
  • Protein Kinase Inhibitors / metabolism
  • Proteomics

Substances

  • Protein Kinase Inhibitors
  • Adenosine Triphosphate
  • Fusion Proteins, bcr-abl