Allosteric Inhibition of Bcr-Abl Kinase by High Affinity Monobody Inhibitors Directed to the Src Homology 2 (SH2)-Kinase Interface.

@article{Wojcik2016AllostericIO,
  title={Allosteric Inhibition of Bcr-Abl Kinase by High Affinity Monobody Inhibitors Directed to the Src Homology 2 (SH2)-Kinase Interface.},
  author={John Wojcik and Allan Joaquim Lamontanara and Grzegorz Grabe and Akiko Koide and Louesa R Akin and Barbara Gerig and Oliver Hantschel and Shohei Koide},
  journal={The Journal of biological chemistry},
  year={2016},
  volume={291 16},
  pages={8836-47}
}
Bcr-Abl is a constitutively active kinase that causes chronic myelogenous leukemia. We have shown that a tandem fusion of two designed binding proteins, termed monobodies, directed to the interaction interface between the Src homology 2 (SH2) and kinase domains and to the phosphotyrosine-binding site of the SH2 domain, respectively, inhibits the Bcr-Abl kinase activity. Because the latter monobody inhibits processive phosphorylation by Bcr-Abl and the SH2-kinase interface is occluded in the… CONTINUE READING

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Myeloid Leukemia, ChronicAssociated with malfunction of gene productBCR protein, human
Bcr - Abl is a constitutively active kinase that causes chronic myelogenous leukemia .
Bcr - Abl is a constitutively active kinase that causes chronic myelogenous leukemia .
Bcr - Abl is a constitutively active kinase that causes chronic myelogenous leukemia .
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