title: A membrane-tethering pepducin that inhibits formyl peptide receptor 2-induced signaling.
abstract: Since formyl peptide receptor 2 (FPR2) plays a key role in the regulation of innate immune response and inflammation, it has been a hot topic to develop molecules which inhibit FPR2-induced cellular responses. In this study, we investigated the effect of an FPR2-derived pepducin in human neutrophils and human umbilical vein endothelial cells (HUVECs). The pepducin (F2pal-12) selectively inhibited FPR2 agonists (MMK-1 and serum amyloid A)-stimulated neutrophil chemotaxis. MMK-1-stimulated superoxide anion production was also inhibited by F2pal-12. HUVECs also express FPR2; FPR2 agonists-stimulated HUVECs migration and tube formation were also selectively inhibited by F2pal-12 but not by scrambled control pepducin. Since FPR2 mediates inflammatory response by inducing chemotactic migration of inflammatory cells, F2pal-12 can be used as a useful material to modulate FPR2-mediated inflammatory responses.
authors.forename: Ha Young
authors.initials: HY
authors.lastname: Lee
authors.forename: Hazzy
authors.initials: H
authors.lastname: Kim
authors.forename: Sun Young
authors.initials: SY
authors.lastname: Lee
authors.forename: Young Su
authors.initials: YS
authors.lastname: Jung
authors.forename: Sang Doo
authors.initials: SD
authors.lastname: Kim
authors.forename: Yoe-Sik
authors.initials: YS
authors.lastname: Bae
mesh_terms: D000595:Amino Acid Sequence; D002465:Cell Movement / Q000187:drug effects; D002478:Cells, Cultured; D002634:Chemotaxis, Leukocyte / Q000187:drug effects; D003627:Data Interpretation, Statistical; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects; D006801:Humans; D055666:Lipopeptides / Q000494:pharmacology*; D008870:Microtubules / Q000187:drug effects; D008969:Molecular Sequence Data; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism; D044042:Receptors, Formyl Peptide / Q000819:agonists / Q000037:antagonists & inhibitors*; D044067:Receptors, Lipoxin / Q000819:agonists / Q000037:antagonists & inhibitors*; D015398:Signal Transduction / Q000187:drug effects*; D013481:Superoxides / Q000378:metabolism
chemical_list: C000588489:F2pal-12 pepducin; C105101:FPR2 protein, human; D055666:Lipopeptides; D044042:Receptors, Formyl Peptide; D044067:Receptors, Lipoxin; D013481:Superoxides