A myristoylated pseudosubstrate peptide of PKC-zeta induces degranulation in HMC-1 cells independently of PKC-zeta activity

Life Sci. 2008 Mar 26;82(13-14):733-40. doi: 10.1016/j.lfs.2008.01.005. Epub 2008 Jan 26.

Abstract

Mast cells play a central role in allergic disease and host defense against several pathogens through the release of various bioactive compounds via degranulation. In this study, we found that a myristoylated pseudosubstrate of PKC-zeta (zeta-PS; myristoyl-SIYRRGARRWRKL, a PKC-zeta inhibitor) regulates mast cell degranulation. zeta-PS increased [Ca+2]i level at nanomolar concentrations in a PKC-zeta activity-independent manner in HMC-1 cells. Moreover, zeta-PS-induced [Ca+2]i generation was completely abrogated by phospholipase C (PLC), IP3 receptor or Galpha i/o inhibitor and zeta-PS potently induced degranulation in HMC-1 cells which was significantly inhibited by pretreating PLC inhibitors or a calcium chelator. Therefore, our results suggest that zeta-PS can induce degranulation in HMC-1 cells by triggering the calcium signal via a PKC-zeta-independent but Galpha i/o, PLC and IP3-dependent pathways.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium / metabolism
  • Calcium Signaling / drug effects
  • Cell Degranulation / drug effects*
  • Cell Degranulation / immunology
  • Cell Line
  • Enzyme Inhibitors / pharmacology*
  • GTP-Binding Protein alpha Subunits, Gi-Go / metabolism
  • Humans
  • Inositol 1,4,5-Trisphosphate Receptors / metabolism
  • Ligands
  • Mast Cells / drug effects*
  • Mast Cells / enzymology
  • Mast Cells / immunology
  • Mast Cells / physiology
  • Microscopy, Confocal
  • Oligopeptides / pharmacology*
  • Peptide Library
  • Protein Kinase C / antagonists & inhibitors
  • Protein Kinase C / physiology*
  • Receptors, G-Protein-Coupled / metabolism
  • Substrate Specificity
  • Type C Phospholipases / metabolism
  • beta-N-Acetylhexosaminidases / metabolism

Substances

  • Enzyme Inhibitors
  • Inositol 1,4,5-Trisphosphate Receptors
  • Ligands
  • Oligopeptides
  • Peptide Library
  • Receptors, G-Protein-Coupled
  • myristoyl-SIYRRGARRWRKL
  • protein kinase C zeta
  • Protein Kinase C
  • Type C Phospholipases
  • beta-N-Acetylhexosaminidases
  • GTP-Binding Protein alpha Subunits, Gi-Go
  • Calcium