title: Activation of human monocytes by a formyl peptide receptor 2-derived pepducin.
abstract: 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.
authors.affiliation: Department of Biological Sciences, Sungkyunkwan University, Suwon, Republic of Korea.
authors.forename: Ha Young
authors.initials: HY
authors.lastname: Lee
authors.forename: Sang Doo
authors.initials: SD
authors.lastname: Kim
authors.forename: Jae Woong
authors.initials: JW
authors.lastname: Shim
authors.forename: Hak Jung
authors.initials: HJ
authors.lastname: Kim
authors.forename: Jae Young
authors.initials: JY
authors.lastname: Kwon
authors.forename: Jong-Min
authors.initials: JM
authors.lastname: Kim
authors.forename: Suk-Hwan
authors.initials: SH
authors.lastname: Baek
authors.forename: Joon Seong
authors.initials: JS
authors.lastname: Park
authors.forename: Yoe-Sik
authors.initials: YS
authors.lastname: Bae
mesh_terms: 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
chemical_list: 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