Protease receptor antagonism to target blood platelet therapies.
Platelet activation and thrombus formation play a central role in ischemic vascular disease. Thrombin, an especially potent physiologic agonist mediating in vivo activation of platelets, acts via a unique family of G-protein-coupled receptors called protease-activated receptors (PARs) with a broad tissue expression. This review focuses on current antiplatelet therapies as well as innovative approaches to targeting PARs in patients with atherothrombotic vascular disease.
University of Michigan Medical School, Departments of Pharmacology and Internal Medicine, Ann Arbor, Michigan, USA.
M
M
Holinstat
Thomas Jefferson University, The Cardeza Foundation for Hematologic Research and the Department of Medicine, Jefferson Medical College, Philadelphia, Pennsylvania, USA.
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PF
Bray
D001792:Blood Platelets / Q000187:drug effects*; D015507:Drugs, Investigational / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008954:Models, Biological; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D011480:Protease Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use*; D018179:Receptors, Thrombin / Q000037:antagonists & inhibitors*; D014652:Vascular Diseases / Q000188:drug therapy*
D015507:Drugs, Investigational; D010975:Platelet Aggregation Inhibitors; D011480:Protease Inhibitors; D018179:Receptors, Thrombin