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Table 5 PAR1 signaling modulators

From: Protease-activated receptors (PARs): mechanisms of action and potential therapeutic modulators in PAR-driven inflammatory diseases

Class Agonist/ Antagonist Name Receptor/Cell/Tissue type Cellular response
Peptide Agonist SFLLRN/−NH2 Human Induces platelet activation [6, 138, 265, 278, 279]
TFLLRN/−NH2 Human Induces platelet activation, enhances endothelial barrier permeability [137, 138, 265]
NPNDKYEPF/−NH2 Human Induces cytoprotective signaling [28, 187]
PRSFLLRN/−NH2 Human Induces platelet activation [86]
Human Induces ERK1/2 activation [280]
Antagonist YFLLRN Human Compets with thrombin and PAR1-AP and prevents platelet activation [278, 279]
Peptidomimetic Antagonist RWJ-56110 Human Blunts thrombin and PAR1-AP effects on platelets and vascular endothelial cells [264, 281, 282]
Human Blocks MMP-1 activaiton in SMCs [87]
RWJ-58259 Guinea pig Blocks thrombin and PAR1-AP platelet activation [215, 283]
Rat Blocks thrombin induced calcium release in AoSMC Inhibits intimal thickening [111, 215, 264, 273]
Mouse Prevents destruction of intestinal barrier [62, 284]
Non-peptide small molecule Antagonist FR17113 Human Blocks PAR1-AP induced platelet activation [285, 286]
Human Inhibits thrombin and PAR1-AP induced ERK1/2 activation [287]
ER129614–06 Human Blocks thrombin and PAR1-AP induced platelet activation [288]
Guinea pig Shows antithrombotic effects [289]
F16357, F16618 Human Blocks PAR1-AP induced platelet activation [290]
Rat Shows antithrombotic effects [291]
SCH79797 Human Blocks thrombin and PAR1-AP induced calcium release and platelet activation [292]
Human, Mouse Induces NETs formation and increases bacterial killing capacity [293]
SCH203009 Human Blocks thrombin and PAR1-AP induced platelet activation [292]
SCH530348 (vorapaxar) Human, Monkey Blocks thrombin and PAR1-AP induced platelet activation [266]
E5555 (atopaxar) Human Blocks thrombin and PAR1-AP induced platelet activation and inhibits thrombus formation [267]
Guinea pig Bleeding time not affected [267, 294]
Q94 Human Blocks thrombin induced calcium release [295]
Mouse Blocks thrombin induced ERK1/2 activation [296]
Pepducin Antagonist P1pal-12 Human Blocks thrombin induced platelet activation [268]
Human Blocks platelet activation [86]
Human Blocks MMP-1 induced endothelial damage [297]
Mouse Reduces lung vascular damage and sepsis lethality [297, 298]
P1-pal7 (PZ-128) Human Blocks MMP-1 induced Akt signaling in cancer cells [150]
Human Blocks platelet activation [86]
Mouse Inhibits tumor growth [280]
Guinea pig Prevents from systemic platelet activation [86]
Parmodulin Antagonist ML161 (Parmodulin-2) Human Blocks thrombin and PAR1-AP induced platelet activation [299]
Human Blocks thrombin induced inflammatory signaling on endothelial cells [269]
Mouse Blocks thrombus formation [300]
Antibiotic Antagonist Doxycycline Human Inhibits thrombin induced cancer cell migration [301, 302]
Human Blocks MMP-1 cleavage [303]
Antibody Antagonist ATAP-2 WEDE Human Blocks thrombin cleavage of PAR1 and thrombin induced calcium release [147]