A pan-specific inhibitor of the polo-box domains of polo-like kinases arrests cancer cells in mitosis.
Playing polo: Small-molecule inhibitors of polo-like kinase 1 are mostly ATP-competitive, and thus face enormous specificity hurdles. This communication explores the concept of inhibiting Plk1 with a small-molecule inhibitor of the protein-protein interactions required for Plk1 function.
Department of Molecular Biology, Max Planck Institute of Biochemistry, Center for Integrated Protein Science Munich, Am Klopferspitz 18, 82152 Martinsried, Germany.
Wolfgang
W
Reindl
Juping
J
Yuan
Andrea
A
Krämer
Klaus
K
Strebhardt
Thorsten
T
Berg
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors*; D045744:Cell Line, Tumor; D018385:Centrosome; D006367:HeLa Cells; D006574:Heterocyclic Compounds, 2-Ring / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008938:Mitosis; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D017434:Protein Structure, Tertiary; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D054852:Small Molecule Libraries; D000097869:Polo-Like Kinase 1
D000970:Antineoplastic Agents; D018797:Cell Cycle Proteins; D006574:Heterocyclic Compounds, 2-Ring; D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; D011518:Proto-Oncogene Proteins; D054852:Small Molecule Libraries; D000097869:Polo-Like Kinase 1; C541733:poloxipan