Activation of human monocytes by a formyl peptide receptor 2-derived pepducin

FEBS Lett. 2010 Sep 24;584(18):4102-8. doi: 10.1016/j.febslet.2010.08.036. Epub 2010 Sep 9.


We synthesized and investigated the effect of formyl peptide receptor 2 (FPR2)-derived pepducins in human monocytes. The FPR2-based cell-penetrating lipopeptide, "pepducin" (F2pal-16), stimulated intracellular calcium increase in human monocytes via pertussis toxin (PTX)-sensitive G-protein and phospholipase C (PLC) activity. From a functional aspect, we showed that F2pal-16 stimulated monocyte chemotaxis. F2pal-16 also stimulated the generation of superoxide anion in human monocytes. Moreover, F2pal-16 dramatically increased the production of several kinds of pro-inflammatory cytokines (CXCL8, CCL2, IL-1β and TNF-α) in human monocytes via NF-κB activation. Since FPR2 plays an important role in immune responses, F2pal-16 can serve as a useful reagent for the study of FPR2-mediated immune modulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Calcium / metabolism
  • Cells, Cultured
  • Chemokine CCL2 / biosynthesis
  • Chemotaxis / drug effects*
  • Chemotaxis / immunology
  • Cytokines / biosynthesis
  • Humans
  • Lipopeptides / chemical synthesis
  • Lipopeptides / pharmacology*
  • Molecular Sequence Data
  • Monocytes / drug effects*
  • Monocytes / immunology
  • NF-kappa B / metabolism
  • Receptors, Formyl Peptide / immunology*
  • Receptors, Lipoxin / immunology*
  • Superoxides / metabolism


  • Chemokine CCL2
  • Cytokines
  • F2pal-16 pepducin
  • FPR2 protein, human
  • Lipopeptides
  • NF-kappa B
  • Receptors, Formyl Peptide
  • Receptors, Lipoxin
  • Superoxides
  • Calcium