Publications by authors named "Motoji Kogushi"
Article Synopsis
- Thrombin activates cellular responses like platelet aggregation and smooth muscle cell proliferation via the PAR-1 receptor.
- The study evaluated E5555, a selective thrombin receptor antagonist, showing it effectively inhibits smooth muscle cell proliferation in both lab and rat models.
- E5555 demonstrated potential in reducing neointimal formation after vascular injury and could be beneficial for treating conditions like restenosis and chronic atherothrombotic disease.
Article Synopsis
- Thrombin is a key player in platelet activation through PAR-1, and E5555 has been identified as a potent antagonist of this receptor, effectively blocking thrombin’s action.
- E5555 demonstrates strong inhibition of platelet aggregation induced by thrombin and TRAP in both humans and guinea pigs, but does not affect aggregation caused by ADP or collagen.
- In guinea pig models, E5555 showed significant antithrombotic effects without increasing bleeding time, suggesting its potential as a treatment for atherothrombotic diseases.
E5555 is a potent protease-activated receptor (PAR-1) antagonist targeting the G-coupled receptor and modulating thrombin-platelet-endothelial interactions. The drug is currently being tested in phase II trials in patients with coronary artery disease (CAD) and has potential antithrombotic and anti-inflammatory benefits. We investigated the in-vitro effects of E5555 on platelet function beyond PAR-1 blockade in healthy volunteers and CAD patients treated with aspirin (ASA) with or without clopidogrel.
View Article and Find Full Text PDF