FAK inhibitors induce cell multinucleation and dramatically increase pro-tumoral cytokine expression in RAW 264.7 macrophages

FEBS Lett. 2017 Dec;591(23):3861-3871. doi: 10.1002/1873-3468.12895. Epub 2017 Nov 24.

Abstract

Macrophages are abundant in the tumor microenvironment. They are highly plastic and able to acquire pro-tumoral phenotypes in response to microenvironmental stimuli. When we treated RAW 264.7 macrophages with inhibitors of various oncogenic pathways, we found that the focal adhesion kinase (FAK) inhibitors PF573228 and TAE226 could induce cell multinucleation by suppressing furrowing and cytokinesis. This failure in cytokinesis involves Rac1, whose activity is elevated by FAK inhibitors, and the p21-activated kinases, comprising the downstream effectors of Rac. We also investigated the influence of cell multinucleation on macrophage physiology in RAW 264.7 cells. This is the first study to report that FAK inhibitors suppress furrow ingression and early cytokinesis. Of note, we found that FAK inhibitors caused a dramatic increase in pro-tumoral cytokines in multinuclear cells, suggesting the potential to convert macrophages into pro-tumoral phenotypes.

Keywords: FAK inhibitor; cytokinesis failure; fluorescein isothiocyanate; macrophage; multinuclear cell; pro-tumoral cytokine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Nucleus / drug effects
  • Cell Nucleus / ultrastructure
  • Cytokines / metabolism
  • Cytokinesis / drug effects
  • Cytokinesis / physiology
  • Focal Adhesion Kinase 1 / antagonists & inhibitors*
  • HCT116 Cells
  • Humans
  • Macrophages / drug effects*
  • Macrophages / physiology
  • Macrophages / ultrastructure
  • Mice
  • Morpholines / pharmacology
  • Neuropeptides / metabolism
  • Phenotype
  • Protein Kinase Inhibitors / pharmacology
  • Quinolones / pharmacology
  • RAW 264.7 Cells
  • Sulfones / pharmacology
  • Tumor Microenvironment / drug effects
  • Tumor Microenvironment / physiology
  • rac1 GTP-Binding Protein / metabolism

Substances

  • 6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one
  • Cytokines
  • Morpholines
  • Neuropeptides
  • Protein Kinase Inhibitors
  • Quinolones
  • Rac1 protein, mouse
  • Sulfones
  • TAE226
  • Focal Adhesion Kinase 1
  • Ptk2 protein, mouse
  • rac1 GTP-Binding Protein