Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.

@article{Johnson2007PharmacologicalAF,
  title={Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.},
  author={Eric F Johnson and Kent D. Stewart and Keith W. Woods and Vincent L. Giranda and Yan Yun Luo},
  journal={Biochemistry},
  year={2007},
  volume={46 33},
  pages={
          9551-63
        }
}
PLK1 (polo-like kinase 1) is a key mitotic kinase and a therapeutic target in the treatment of proliferative diseases. Here we investigate the relative substrate specificity and pharmacological relatedness of PLK1, -2, -3, and -4 that together comprise a conserved family of Ser/Thr kinases (PLK family). We report consensus substrate sequences for PLK2, -3, and -4 and an expanded consensus sequence for PLK1, which we use to design an optimal peptide substrate, PLKtide. We report inhibitory… CONTINUE READING

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