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Table 7 PAR4 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 GYPGQV/−NH2 Human, Rat Induces platelet activation [144]
GYPGKF/−NH2 Human, Rat Induces platelet activation [144]
AYPGKF/−NH2 Human, Mouse Induces platelet activation [145]
Peptidomimetic Antagonist tc-YGPKF Rat Blocks thrombin and PAR4-AP induced platelets aggregation [321]
Non-peptide small molecule Antagonist YD-3 Human Blocks thrombin induced platelet activation [282, 322,323,324,325]
Mouse, Rat, Rabbit Blocks thrombin and PAR4-AP induced platelets activation [323,324,325]
ML-354 Human Blocks PAR4-AP induced platelet activation [326,327,328]
BMS-986120 Human Blocks PAR4-AP induced calcium release and platelet activation [329]
Human Blocks thrombus formation at high shear stress [277]
Monkey Blocks platelet activation [329]
Pepducin Antagonist P4pal-10 Human, Mouse Blocks thrombin and PAR4-AP induced platelet activation [268]
Rat Blocks thrombin and PAR4-AP induced platelets activation [330]
P4pal-i1 Human Blocks PAR4 induced platelets activation [150]