Activation of human monocytes by a formyl peptide receptor 2-derived pepducin.
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.
Lee
Ha Young
HY
Department of Biological Sciences, Sungkyunkwan University, Suwon, Republic of Korea.
Kim
Sang Doo
SD
Shim
Jae Woong
JW
Kim
Hak Jung
HJ
Kwon
Jae Young
JY
Kim
Jong-Min
JM
Baek
Suk-Hwan
SH
Park
Joon Seong
JS
Bae
Yoe-Sik
YS
D000595:Amino Acid Sequence; D002118:Calcium / Q000378:metabolism; D002478:Cells, Cultured; D018932:Chemokine CCL2 / Q000096:biosynthesis; D002633:Chemotaxis / Q000187:drug effects* / Q000276:immunology; D016207:Cytokines / Q000096:biosynthesis; D006801:Humans; D055666:Lipopeptides / Q000138:chemical synthesis / Q000494:pharmacology*; D008969:Molecular Sequence Data; D009000:Monocytes / Q000187:drug effects* / Q000276:immunology; D016328:NF-kappa B / Q000378:metabolism; D044042:Receptors, Formyl Peptide / Q000276:immunology*; D044067:Receptors, Lipoxin / Q000276:immunology*; D013481:Superoxides / Q000378:metabolism
D018932:Chemokine CCL2; D016207:Cytokines; C552958:F2pal-16 pepducin; C105101:FPR2 protein, human; D055666:Lipopeptides; D016328:NF-kappa B; D044042:Receptors, Formyl Peptide; D044067:Receptors, Lipoxin; D013481:Superoxides; D002118:Calcium