Table 7 PAR4 signaling modulators
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 | |||
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] |