Abstract
Objective To study the effects of the myristoyl-glycine modified peptide which derived from the second intracellular loop of sphingosine 1-phosphate receptor 3 (S1PR3) on activation of mitogen-activated protein kinases (MAPKs) pathway. Methods The phosphorylation levels of JNK and ERK in THP-1 cells were detected by western blot after GPS-725.017 stimulation. Statistical data analysis was conducted by multivariate analysis of variance. Results Western blot showed that 10 min after 30 μmol/L or 50 μmol/L GPS-725.017 stimulated, phosphorylation of ERK significantly increased in comparison with the solvent-treated group [30 μmol/L group: (3.10±0.27)vs.(7.98±0.45), P<0.01; 50 μmol/L group: (4.78±0.44)vs.(25.98±2.32), P<0.01]; after 50 μmol/L GPS-725.017 stimulated THP-1 cells for 5 min, 10 min, 20 min or 30 min, p-ERK or p-JNK level raised at different time points (P< 0.01vs.solvent group). Conclusions GPS-725.017, a kind of myristoyl-glycine modified peptide derived from S1PR3, could traverse cytomembrane and activate MAPKs pathway. This study provides an implication of targeting S1PR3 for clinical therapy on inflammatory diseases or sepsis. Key words: S1PR3; G protein; Myristoyl-glycine; GPS-725.017; MAPKs; Monocyte; Inflammation; Sepsis
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