A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators

Mol Cancer Ther. 2011 Feb;10(2):242-54. doi: 10.1158/1535-7163.MCT-10-0720. Epub 2011 Jan 7.

Abstract

High-content screening is increasingly used to elucidate changes in cellular biology arising from treatment with small molecules and biological probes. We describe a cell classifier for automated analysis of multiparametric data from immunofluorescence microscopy and characterize the phenotypes of 41 cell-cycle modulators, including several protein kinase inhibitors in preclinical and clinical development. This method produces a consistent assessment of treatment-induced phenotypes across experiments done by different biologists and highlights the prevalence of nonuniform and concentration-dependent cellular response to treatment. Contrasting cell phenotypes from high-content screening to kinase selectivity profiles from cell-free assays highlights the limited utility of enzyme potency ratios in understanding the mechanism of action for cell-cycle kinase inhibitors. Our cell-level approach for assessing phenotypic outcomes is reliable, reproducible and capable of supporting medium throughput analyses of a wide range of cellular perturbations.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Cell Cycle / drug effects*
  • Cell Proliferation / drug effects
  • Cells / cytology*
  • Cells / drug effects*
  • Decision Trees
  • Dose-Response Relationship, Drug
  • HCT116 Cells
  • Humans
  • Microscopy, Fluorescence
  • Microtubules / metabolism
  • Phenotype*
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / metabolism
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Serine-Threonine Kinases / metabolism
  • Reproducibility of Results

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Protein Serine-Threonine Kinases