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Activation of human monocytes by a formyl peptide receptor 2‐derived pepducin
Author(s) -
Lee Ha Young,
Kim Sang Doo,
Shim Jae Woong,
Kim Hak Jung,
Kwon Jae Young,
Kim Jong-Min,
Baek Suk-Hwan,
Park Joon Seong,
Bae Yoe-Sik
Publication year - 2010
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2010.08.036
Subject(s) - pertussis toxin , monocyte , lipopeptide , superoxide , chemotaxis , chemistry , receptor , interleukin 8 , immune system , phospholipase c , intracellular , peptide , formyl peptide receptor , ccl2 , phospholipase a2 , inflammation , microbiology and biotechnology , chemokine , biochemistry , biology , immunology , g protein , enzyme , genetics , bacteria
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.