Structural mechanism for STI-571 inhibition of abelson tyrosine kinase.
@article{Schindler2000StructuralMF, title={Structural mechanism for STI-571 inhibition of abelson tyrosine kinase.}, author={T. 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 } }
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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References
SHOWING 1-10 OF 27 REFERENCES
Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor.
- Biology, Medicine
- Molecular cell
- 1999
- 388
Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.
- Biology, Medicine
- Science
- 1997
- 1,093
Crystal structures of c-Src reveal features of its autoinhibitory mechanism.
- Biology, Medicine
- Molecular cell
- 1999
- 787
- PDF
An intramolecular SH3-domain interaction regulates c-Abl activity
- Medicine, Biology
- Nature Genetics
- 1998
- 213
Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr–Abl positive cells
- Chemistry, Medicine
- Nature Medicine
- 1996
- 3,455
- PDF
Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives
- Chemistry
- 1997
- 200
N‐terminal mutations activate the leukemogenic potential of the myristoylated form of c‐abl.
- Biology, Medicine
- The EMBO journal
- 1989
- 228
The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase.
- Medicine, Biology
- Chemistry & biology
- 1997
- 245
Autoregulatory Mechanisms in Protein-tyrosine Kinases*
- Chemistry, Medicine
- The Journal of Biological Chemistry
- 1998
- 306
- PDF