Antagonist | Targeted cell | Response of cell |
---|---|---|
PAR-1 | ||
SCH 79797 | HUVEC [165]; HDF [166]; MC [29] | Block thrombin induced CX3CL1 [165]; inhibit plasmin-induced IL-8, PGE [166]; inhibit trypsin and tryptase induced IL-4 release [29] |
BMS 200261 | PL [114] | Inhibit PAR-1 activation in response to thrombin [114]; |
RWJ-56110 [122, 167]; RWJ-58259 [123] | HSC [167]; HVC, PL [112, 113] | Reduced liver type I collagen [167], reduced liver calcium mobilization, and cellular functions (platelet aggregation and cell proliferation [112, 113]) |
| ||
PAR-2 | ||
FSLLRY-NH2 | HUVEC [108]; Astr [111]; MC [20, 29, 31, 32] | Inhibit trypsin-induced IL-8 [108]; alleviate IL-6 and TNF-α secretion [111]; inhibit trypsin and tryptase induced IL-4 release [20, 29, 31]; inhibit tryptase induced IL-13 release [32] |
ENMD-1068 | Eos [168] | Abolish tryptase-induced eosinophil recruitment [168] |
GB88 | HTEC [102]; HT29, A549, Panc-1, MKN1, MKN45, MDA-MB231, HUVEC [117]; Mac, MC [169] | Block PAR-2 agonist-induced increases in GM-CSF, IL-6, IL-8, and TNF-α [102]; ameliorate macrophage invasion and MC degranulation [169]; inhibit PAR-2 activated Ca(2+) release induced by trypsin or synthetic peptide and nonpeptide agonists [117] |
| ||
PAR-4 | ||
Pepducin P4pal-10 | Neu [115] | Diminish neutrophil migration mediated by neutrophil expressed PAR-4 [115] |
PBMC: peripheral blood mononuclear cells; A549: A549 epithelial cells; Mon: monocyte; TC: T cell; HPDF: human primary dermal fibroblast; CHAEC: cultured human airway epithelial cell; EnC: endothelial cell; HBEC: human bronchial epithelial cell; Neu: neutrophil; Astr: astrocytes; HPBF: human primary bronchial fibroblasts; Eos: eosinophil; MC: mast cell; HUVEC: human umbilical vein endothelial cell; AEC: airway epithelial cells; MH-S: alveolar macrophage cell lines; RAW264.7: peritoneal macrophage cell lines; PHKC: primary human keratinocyte; HTEC: kidney tubular epithelial cells; Kerat: keratinocyte; BEAS-2B: human airway epithelial cell line BEAS-2B; Calu-3: human airway epithelial cell line Calu-3; HDF: human dental pulp fibroblast-like cells; PL: platelet; HSC: hepatic stellate cell; HVC: human vascular cell; HT29: human colon adenocarcinoma cell line; Panc-1: pancreas epithelioid carcinoma line Panc-1; MKN1: human gastric carcinoma cell line MKN1; MKN45: human gastric carcinoma cell line MKN45; MDA-MB231: breast adenocarcinoma cell line MDA-MB231; Mac: macrophage; IL: interleukin; MCP-1: monocyte chemoattractant protein-1; MMP: matrix metalloproteinase; VCAM: vascular cell adhesion molecule; VEGF: vascular endothelial growth factor; PG: prostaglandin; LF: lactoferrin; TNF: tumor necrosis factor; ROS: reactive oxygen species; G-CSF: granulocyte colony-stimulating factor; cys-LT: cysteinyl leukotrienes; MUC5AC: mucin5AC; GM-CSF: granulocyte-macrophage colony-stimulating factor; TSLP: thymic stromal lymphopoietin; SOD: superoxide; His: histamine; ICAM: intercellular adhesion molecule.