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

Biochemistry. 2007 Aug 21;46(33):9551-63. doi: 10.1021/bi7008745. Epub 2007 Jul 27.

Abstract

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 activity for the entire PLK family across a diverse set of small-molecule ATP-competitive inhibitors including several clinical compounds. With respect to both substrate and ATP-site specificity, highest similarity is observed between PLK2 and PLK3, PLK1 is next most similar, and PLK4 is least similar. Further, we have identified and report time-dependent inhibition by two potent and selective PLK inhibitors.

MeSH terms

  • Adenosine Triphosphate / chemistry
  • Amino Acid Sequence
  • Androstadienes / chemistry
  • Binding Sites
  • Cell Cycle Proteins / antagonists & inhibitors*
  • Cell Cycle Proteins / chemistry*
  • Humans
  • Models, Molecular
  • Molecular Sequence Data
  • Peptide Library
  • Polo-Like Kinase 1
  • Protein Conformation
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Protein Serine-Threonine Kinases / chemistry*
  • Proto-Oncogene Proteins / antagonists & inhibitors*
  • Proto-Oncogene Proteins / chemistry*
  • Pteridines / chemistry
  • Substrate Specificity
  • Wortmannin

Substances

  • Androstadienes
  • BI 2536
  • Cell Cycle Proteins
  • Peptide Library
  • Protein Kinase Inhibitors
  • Proto-Oncogene Proteins
  • Pteridines
  • Adenosine Triphosphate
  • Protein Serine-Threonine Kinases
  • Wortmannin