SLIGKV-NH2 is a protease-activated receptor 2 (PAR2) agonist with an IC50 value of 10.1µM[1]. SLIGKV-NH2 effectively increases intracellular Ca2+ levels, with EC50 values of 109µM, 23.2µM, and 7.46µM in human umbilical vein endothelial cells (HUVECs), A549, and MDA-MB-231 cells, respectively[2]. SLIGKV-NH2 activates PAR2, thereby inducing a strong pro-inflammatory response, and increases the levels of IL-6, IL-8, GM-CSF, and TNF-α[3]. SLIGKV-NH2 has been widely used in immunological research to induce the release of histamine by colonic mast cells[4].
In vitro, SLIGKV-NH2 treatment (50µM) for 24 hours promoted the proliferation of HepG2 cells and enhanced the activity of the ERK/AP-1 pathway[5]. Incubation with 100µM SLIGKV-NH2 for 16 hours promoted the secretion of IL-6 by human T cells[6]. Treatment with 100µM SLIGKV-NH2 for 24 hours downregulated expression of involucrin in HaCaT keratinocytes[7].
In vivo, Intrathecal injection of SLIGKV-NH2 at a dose of 8µg induced thermal hyperalgesia and reduced paw withdrawal latency (PWL) in rats within 4 hours[8].
References:[1] Maryanoff B E, Santulli R J, McComsey D F, et al. Protease-activated receptor-2 (PAR-2): structure-function study of receptor activation by diverse peptides related to tethered-ligand epitopes[J]. Archives of biochemistry and biophysics, 2001, 386(2): 195-204.
[2] Stahn S, Thelen L, Albrecht I M, et al. Teleocidin A2 inhibits human proteinase‐activated receptor 2 signaling in tumor cells[J]. Pharmacology Research & Perspectives, 2016, 4(4): e00230.
[3] Vesey D A, Suen J Y, Seow V, et al. PAR2-induced inflammatory responses in human kidney tubular epithelial cells[J]. American Journal of Physiology-Renal Physiology, 2013, 304(6): F737-F750.
[4] He S H, He Y S, Xie H. Activation of human colon mast cells through proteinase activated receptor-2[J]. World Journal of Gastroenterology, 2004, 10(3): 327.
[5] Xie L, Zheng Y, Li X, et al. Enhanced proliferation of human hepatoma cells by PAR-2 agonists via the ERK/AP-1 pathway[J]. Oncology Reports, 2012, 28(5): 1665-1672.
[6] Li T, He S. Induction of IL‐6 release from human T cells by PAR‐1 and PAR‐2 agonists[J]. Immunology and cell biology, 2006, 84(5): 461-466.
[7] Joo Y A, Chung H, Yoon S, et al. Skin barrier recovery by protease-activated receptor-2 antagonist lobaric acid[J]. Biomolecules & therapeutics, 2016, 24(5): 529.
[8] Mrozkova P, Spicarova D, Palecek J. Hypersensitivity induced by activation of spinal cord PAR2 receptors is partially mediated by TRPV1 receptors[J]. PLoS One, 2016, 11(10): e0163991.
















