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

Thorsten Schindler; W. Bornmann; P. Pellicena; W. Miller; B. Clarkson; J. Kuriyan

DOI:10.1126/SCIENCE.289.5486.1938

Corpus ID: 957274

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

@article{Schindler2000StructuralMF,
  title={Structural mechanism for STI-571 inhibition of abelson tyrosine kinase.},
  author={Thorsten Schindler and W. Bornmann and P. Pellicena and W. Miller and B. Clarkson and J. Kuriyan},
  journal={Science},
  year={2000},
  volume={289 5486},
  pages={
          1938-42
        }
}

Thorsten Schindler, W. Bornmann, +3 authors J. Kuriyan

Published 2000

Medicine, Biology

Science

The inadvertent activation of the Abelson tyrosine kinase (Abl) causes chronic myelogenous leukemia (CML. [...] Key Result 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 that in active protein kinases, as well as in the inactive form of the closely related Src kinases. These results suggest that compounds that exploit the distinctive inactivation…Expand Abstract

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