Table 8.
Ligand | Origin | Selectivity | Cells | Effects | Ref. | Potency |
---|---|---|---|---|---|---|
WKYMVm | Peptide library | FPR2 | Neutrophils | increase in Ca++ concentration; NADPH oxidase activation; cPLA2-mediated arachidonic acid release; increase of LTB4 production | [115,120] | pEC50 = 8.70 |
Monocytes | chemotaxis; p125FAK, Pyk, MEK, ERKs, Akt and RhoA phosphorylation; NADPH oxidase activation; PKC and PLD activation | [118,121] | EC50 = 50 nM | |||
Eosinophils | ERKs phosphorylation; NADPH oxidase activation; PI3K/ERK pathway | [122] | ||||
U937 | ERKs phosphorylation; G0/PI3K/Ras/Raf-1 pathway; cPLA and PLD activation; LPA formation; Ca++ influx | [123,124] | pEC50 = 10.13 | |||
NK | chemotaxis in IL-2-activated NK cells; ERKs, p38MAPK and JNK activation | [125] | EC50 = 9.2 nM | |||
IMR90 | ERKs activation; p47phox translocation; NADPH oxidase, PKCα and PKCδ activation | [126,127] | Kd = 155,99 nM | |||
CaLu-6 | EGFR transactivation, p47phox phosphorylation, NADPH oxidase activation; c-Src activation; STAT3 pathway; cell growth | [128] | - | |||
U87 | ERKs, p38MAPK and JNK activation; c-Src and PLCβ activation; GFAP and IL-1α upregulation; IKK phosphorylation; PI3K activation; Ca++ influx | [129–131] | EC50 = 50–100 nM | |||
iDC | downregulation of CCR5; PKC activation | [132] | ||||
Osteosarcoma | downregulation of CXCR4 | [133] | ||||
Mouse model | Anti-apoptosis; enhanced production of IFN-γ, IL-12, IL-17 and TGF-β; reduced production of TNF-α, IL-1β and IL-6 | [134] | ||||
FPR2/RBL-2H3 | ERKs phosphorylation; STAT3 serine phosphorylation; PLD activation | [135] |
LPA, lysophosphatidic acid; IKK, inhibitory-κB kinase; pEC50, negative logarithm of the EC50.