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

作者：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^*

来源：FEBS Letters, 2010, 584(18): 4102-4108.

DOI：10.1016/j.febslet.2010.08.036

• FPR2
• Pepducin
• Monocytes
• Chemotaxis
• Pertussis toxin-sensitive G-protein
• Cytokine

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-1 beta and TNF-alpha) in human monocytes via NF-kappa B 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.

• 出版日期2010-9-24