Structural mechanism for STI-571 inhibition of abelson tyrosine kinase.

@article{Schindler2000StructuralMF,
  title={Structural mechanism for STI-571 inhibition of abelson tyrosine kinase.},
  author={Thomas Schindler and William G. Bornmann and Patricia Pellicena and W Todd Miller and Bayard Clarkson and John Kuriyan},
  journal={Science},
  year={2000},
  volume={289 5486},
  pages={1938-42}
}
The inadvertent activation of the Abelson tyrosine kinase (Abl) causes chronic myelogenous leukemia (CML). A small-molecule inhibitor of Abl (STI-571) is effective in the treatment of CML. We report the crystal structure of the catalytic domain of Abl, complexed to a variant of STI-571. Critical to the binding of STI-571 is the adoption by the kinase of an inactive conformation, in which a centrally located "activation loop" is not phosphorylated. The conformation of this loop is distinct from… CONTINUE READING
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Single-letter abbreviations for the amino acid residues

  • A Ala, C Cys, +17 authors Y Tyr.
  • R E P O R T S www.sciencemag.org SCIENCE VOL
  • 2000
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  • J. M. Lionberger, M. B. Wilson, T. E. Smithgall, J. Biol
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