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}
}

• Thomas Schindler, William G. Bornmann, +3 authors John Kuriyan
• Published 2000 in Science

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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