Selective inhibitors of Kv11.1 regulate IL-6 expression by macrophages in response to TLR/IL-1R ligands

ScientificWorldJournal. 2010 Aug 17:10:1580-96. doi: 10.1100/tsw.2010.155.

Abstract

The mechanism by which the platelet-endothelial cell adhesion molecule PECAM-1 regulates leukodiapedesis, vascular endothelial integrity, and proinflammatory cytokine expression in vivo is not known. We recently identified PECAM-1 as a negative regulator of Kv11.1, a specific voltage-gated potassium channel that functioned in human macrophages to reset a resting membrane potential following depolarization. We demonstrate here that dofetilide (DOF), a selective inhibitor of the Kv11.1 current, had a profound inhibitory effect on neutrophil recruitment in mice following TLR/IL-1R-elicited peritonitis or intrascrotal injection of IL-1 Beta, but had no effect on responses seen with TNF alpha. Furthermore, inhibitors of Kv11.1 (DOF, E4031, and astemizole), but not Kv1.3 (margatoxin), suppressed the expression of IL-6 and MCP-1 cytokines by murine resident peritoneal macrophages, while again having no effect on TNF alpha. In contrast, IL-6 expression by peritoneal mesothelial cells was unaffected. Using murine P388 cells, which lack endogenous C/EBP Beta expression and are unresponsive to LPS for the expression of both IL-6 and MCP-1, we observed that DOF inhibited LPS-induced expression of IL-6 mRNA following ectopic expression of wild-type C/EBP Beta, but not a serine-64 point mutant. Finally, DOF inhibited the constitutive activation of cdk2 in murine peritoneal macrophages; cdk2 is known to phosphorylate C/EBP Beta at serine-64. Taken together, our results implicate a potential role for Kv11.1 in regulating cdk2 and C/EBP Beta activity, where robust transactivation of both IL-6 and MCP-1 transcription is known to be dependent on serine-64 of C/EBP Beta. Our data might also explain the altered phenotypes displayed by PECAM-1 knockout mice in several disease models.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • CCAAT-Enhancer-Binding Protein-beta / metabolism
  • Cells, Cultured
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels / antagonists & inhibitors*
  • Ether-A-Go-Go Potassium Channels / metabolism
  • Female
  • Interleukin-6 / genetics
  • Interleukin-6 / metabolism*
  • Ligands
  • Macrophages / cytology
  • Macrophages / drug effects*
  • Macrophages / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Neutrophils / drug effects
  • Neutrophils / metabolism
  • Peritonitis / metabolism
  • Peritonitis / prevention & control
  • Phenethylamines / pharmacology*
  • Platelet Endothelial Cell Adhesion Molecule-1 / genetics
  • Platelet Endothelial Cell Adhesion Molecule-1 / metabolism
  • Potassium Channel Blockers / pharmacology
  • Receptors, Interleukin-1 / metabolism
  • Sulfonamides / pharmacology*
  • Toll-Like Receptors / metabolism

Substances

  • CCAAT-Enhancer-Binding Protein-beta
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels
  • Interleukin-6
  • KCNH2 protein, human
  • Ligands
  • Phenethylamines
  • Platelet Endothelial Cell Adhesion Molecule-1
  • Potassium Channel Blockers
  • Receptors, Interleukin-1
  • Sulfonamides
  • Toll-Like Receptors
  • dofetilide