Study of the activating effects of myristoyl-glycine modified peptide which derived from S1PR3 / 中华急诊医学杂志

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 mitogenactivated 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 S1 PR3,could traverse cytomembrane and activate MAPKs pathway.This study provides an implication of targeting S1PR3 for clinical therapy on inflammatory diseases or sepsis.