Selective inhibition of Aurora A and B kinases effectively induces cell cycle arrest in t(8;21) acute myeloid leukemia

Biomed Pharmacother. 2019 Sep:117:109113. doi: 10.1016/j.biopha.2019.109113. Epub 2019 Jun 14.

Abstract

The fusion gene AML1-ETO initially dysregulates various cell cycle molecules in t(8;21) acute myeloid leukemia. Aurora kinases have shown great promise in treating tumors. However, the efficacy of Aurora kinase (AURK) A and B inhibition in t(8;21) AML remains unclear. We found that AURK-A inhibitor Alisertib and AURK-B inhibitor Barasertib strongly inhibited the growth and proliferation of t(8;21) AML cells. The quantity and size of cell colonies were markedly decreased after a 14-d drug exposure. The cell cycle distribution was blocked at the G2/M phase in both dose- and time-dependent manner. The expression of p53 family and cdc2-p34 significantly changed as well. Notably, we found that t(8;21) AML cells are more sensitive to Aurora B inhibition. In each set of experiments, Barasertib took less time or a lower concentration to achieve similar efficacy. Taken together, our data highlighted the potential role of Aurora kinases as promising cell cycle targets for the treatment of t(8;21) AML and hereby provided a theoretical basis to guide relevant clinical trials.

Keywords: AML-ETO; Acute myeloid leukemia; Alisertib; Aurora kinase; Barasertib.

MeSH terms

  • Aurora Kinase A / antagonists & inhibitors*
  • Aurora Kinase A / metabolism
  • Aurora Kinase B / antagonists & inhibitors*
  • Aurora Kinase B / metabolism
  • Azepines / pharmacology
  • Cell Cycle Checkpoints / drug effects*
  • Cell Cycle Proteins / metabolism
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Chromosomes, Human, Pair 21 / genetics*
  • Chromosomes, Human, Pair 8 / genetics*
  • Humans
  • Leukemia, Myeloid, Acute / genetics
  • Leukemia, Myeloid, Acute / pathology*
  • Organophosphates / pharmacology
  • Protein Kinase Inhibitors / pharmacology*
  • Pyrimidines / pharmacology
  • Quinazolines / pharmacology
  • Time Factors
  • Translocation, Genetic*
  • Tumor Stem Cell Assay

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
  • Azepines
  • Cell Cycle Proteins
  • MLN 8237
  • Organophosphates
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Quinazolines
  • Aurora Kinase A
  • Aurora Kinase B