Binucleine 2, an isoform-specific inhibitor of Drosophila Aurora B kinase, provides insights into the mechanism of cytokinesis

ACS Chem Biol. 2010 Nov 19;5(11):1015-20. doi: 10.1021/cb1001685.

Abstract

Aurora kinases are key regulators of cell division and important targets for cancer therapy. We report that Binucleine 2 is a highly isoform-specific inhibitor of Drosophila Aurora B kinase, and we identify a single residue within the kinase active site that confers specificity for Aurora B. Using Binucleine 2, we show that Aurora B kinase activity is not required during contractile ring ingression, providing insight into the mechanism of cytokinesis.

Publication types

  • Letter
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Aurora Kinase B
  • Aurora Kinases
  • Cell Cycle Proteins / antagonists & inhibitors
  • Cell Cycle Proteins / chemistry
  • Cell Cycle Proteins / physiology*
  • Cytokinesis / drug effects
  • Cytokinesis / physiology*
  • Drosophila Proteins / antagonists & inhibitors
  • Drosophila Proteins / chemistry
  • Drosophila Proteins / physiology*
  • Drosophila melanogaster / cytology*
  • Drosophila melanogaster / drug effects
  • Drosophila melanogaster / enzymology*
  • Isoenzymes / antagonists & inhibitors
  • Isoleucine / chemistry
  • Molecular Sequence Data
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Protein-Serine-Threonine Kinases / antagonists & inhibitors
  • Protein-Serine-Threonine Kinases / chemistry
  • Protein-Serine-Threonine Kinases / physiology*
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology
  • RNA Interference
  • Schiff Bases / chemistry*
  • Schiff Bases / pharmacology

Substances

  • Cell Cycle Proteins
  • Drosophila Proteins
  • Isoenzymes
  • Protein Kinase Inhibitors
  • Pyrazoles
  • Schiff Bases
  • binucleine 2
  • Isoleucine
  • AurB protein, Drosophila
  • Aurora Kinase B
  • Aurora Kinases
  • Protein-Serine-Threonine Kinases