Structural elements and allosteric mechanisms governing regulation and catalysis of CSK-family kinases and their inhibition of Src-family kinases.

@article{Ia2010StructuralEA,
  title={Structural elements and allosteric mechanisms governing regulation and catalysis of CSK-family kinases and their inhibition of Src-family kinases.},
  author={Kim Kui Ia and Ryan D. Mills and Mohammed I. Hossain and Khai-Chew Chan and Boonyarin Jarasrassamee and Robert N. Jorissen and Heung-Chin Cheng},
  journal={Growth factors},
  year={2010},
  volume={28 5},
  pages={329-50}
}
C-terminal Src kinase (CSK) and CSK-homologous kinase (CHK) are endogenous inhibitors constraining the activity of the oncogenic Src-family kinases (SFKs) in cells. Both kinases suppress SFKs by selectively phosphorylating their consensus C-terminal regulatory tyrosine. In addition to phosphorylation, CHK can suppress SFKs by a unique non-catalytic inhibitory mechanism that involves tight binding of CHK to SFKs to form stable complexes. In this review, we discuss how allosteric regulators… CONTINUE READING

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