Aurora B kinase regulates the postmitotic endoreduplication checkpoint via phosphorylation of the retinoblastoma protein at serine 780

Mol Biol Cell. 2009 Apr;20(8):2218-28. doi: 10.1091/mbc.e08-08-0885. Epub 2009 Feb 18.

Abstract

The phenotypic change characteristic of Aurora B inhibition is the induction of polyploidy. Utilizing specific siRNA duplexes and a selective small molecule inhibitor (AZD1152) to inhibit Aurora B activity in tumor cells, we sought to elucidate the mechanism by which Aurora B inhibition results in polyploidy. Cells treated with AZD1152 progressed through mitosis with misaligned chromosomes and exited without cytokinesis and subsequently underwent endoreduplication of DNA despite activation of a p53-dependent pseudo G1 checkpoint. Concomitant with polyploid cell formation, we observed the appearance of Rb hypophosphorylation, an event that occurred independently of cyclin-dependent kinase inhibition. We went on to discover that Aurora B directly phosphorylates Rb at serine 780 both in vitro and in vivo. This novel interaction plays a critical role in regulating the postmitotic checkpoint to prevent endoreduplication after an aberrant mitosis. Thus, we propose for the first time that Aurora B determines cellular fate after an aberrant mitosis by directly regulating the Rb tumor suppressor protein.

MeSH terms

  • Amino Acid Sequence
  • Aurora Kinase B
  • Aurora Kinases
  • HCT116 Cells
  • Histones / metabolism
  • Humans
  • Mitosis* / drug effects
  • Molecular Sequence Data
  • Organophosphates / pharmacology
  • Phosphorylation / drug effects
  • Phosphoserine / metabolism*
  • Polyploidy*
  • Protein Binding / drug effects
  • Protein Kinase Inhibitors / pharmacology
  • Protein Serine-Threonine Kinases / antagonists & inhibitors
  • Protein Serine-Threonine Kinases / metabolism*
  • Quinazolines / pharmacology
  • Retinoblastoma Protein / chemistry
  • Retinoblastoma Protein / metabolism*
  • Tumor Suppressor Protein p53 / metabolism

Substances

  • 2-((3-((4-((5-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1H-pyrazol-3-yl)amino)quinazolin-7-yl)oxy)propyl)(ethyl)amino)ethyl dihydrogen phosphate
  • Histones
  • Organophosphates
  • Protein Kinase Inhibitors
  • Quinazolines
  • Retinoblastoma Protein
  • Tumor Suppressor Protein p53
  • Phosphoserine
  • AURKB protein, human
  • Aurora Kinase B
  • Aurora Kinases
  • Protein Serine-Threonine Kinases