WKYMVm, a synthetic peptide, is a potent Formyl peptide receptor 2 (FPR2) agonist, exerts an immunoregulatory effect[1]. WKYMVm activates FPR2 to stimulate phagocytes, thereby inducing the chemotaxis and calcium ion influx of phagocytes[2]. WKYMVm has been widely used to promote the homing of endothelial colony-forming cells to stimulate ischemic angiogenesis[3].
In vitro, WKYMVm treatment (10μM) for 1 minute induced the translocation of p47phox and NADPH-dependent superoxide production in serum-deprived human fibroblasts[4]. Treatment with 10μM WKYMVm for 72 hours inhibited the formation of mature osteoclasts induced by RANKL in RAW264.7 cells and reduced the intracellular ROS levels[5]. Treatment with 5μM WKYMVm for 2 hours decreased the lipopolysaccharide (LPS) induced-production of inflammatory cytokines in rat microglial cells, and suppressed the activities of the ERK1/2 and NF-κB p65 signaling pathways[6].
In vivo, WKYMVm administration via subcutaneous injection (8mg/kg) every 2 days for 5 weeks ameliorated high-fat diet (HFD)-induced obesity in mice, reduced food intake, and alleviated HFD-induced histological damage in the liver and adipose tissues[7]. Subcutaneously inject WKYMVm (8mg/kg) once every 12 hours for a total of 60 hours to improved ulcerative colitis in mice triggered by dextran sulphate sodium salt (DSS)[8].
References:
[1] Ma H, Guo X, Wang Z, et al. Therapeutic potential of WKYMVm in diseases[J]. Frontiers in Pharmacology, 2022, 13: 986963.
[2] Le Y, Gong W, Li B, et al. Utilization of two seven-transmembrane, G protein-coupled receptors, formyl peptide receptor-like 1 and formyl peptide receptor, by the synthetic hexapeptide WKYMVm for human phagocyte activation[J]. The Journal of Immunology, 1999, 163(12): 6777-6784.
[3] Heo S C, Kwon Y W, Jang I H, et al. WKYMVm-induced activation of formyl peptide receptor 2 stimulates ischemic neovasculogenesis by promoting homing of endothelial colony-forming cells[J]. Stem cells, 2014, 32(3): 779-790.
[4] Ammendola R, Russo L, De Felice C, et al. Low-affinity receptor-mediated induction of superoxide by N-formyl-methionyl-leucyl-phenylalanine and WKYMVm in IMR90 human fibroblasts[J]. Free Radical Biology and Medicine, 2004, 36(2): 189-200.
[5] Hu J, Li X, Chen Y, et al. The protective effect of WKYMVm peptide on inflammatory osteolysis through regulating NF‐κB and CD9/gp130/STAT3 signalling pathway[J]. Journal of Cellular and Molecular Medicine, 2020, 24(2): 1893-1905.
[6] Zhang W, Chen J, Guo W, et al. WKYMVm/FPR2 alleviates spinal cord injury by attenuating the inflammatory response of microglia[J]. Mediators of inflammation, 2022, 2022(1): 4408099.
[7] Kang J H, Kim H S, Park S H, et al. WKYMVm ameliorates obesity by improving lipid metabolism and leptin signalling[J]. Journal of Cellular and Molecular Medicine, 2023, 27(18): 2782-2791.
[8] Kim S D, Kwon S, Lee S K, et al. The immune-stimulating peptide WKYMVm has therapeutic effects against ulcerative colitis[J]. Experimental & molecular medicine, 2013, 45(9): e40-e40.
















