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Medical Science Monitor Basic Research


eISSN: 1643-3750

Molecular and therapeutical aspects of the blood platelet receptors antagonists

Marcin Różalski, Magdalena Boncler, Bogusława Więcławska, Cezary Watała

Med Sci Monit 1999; 5(2): RA357-375

ID: 505175

Available online:

Published: 1999-03-01

Many new, potent, antiplatelet agents belonging to the group of platelet receptors antagonists became recently available for clinical evaluation and intervention. Amongst platelet inhibitors of a newer generation including inhibitors of platelet adhesion, inhibitors of specific platelet agonist-receptor interactions (antithrombins, fibrinogen receptor antagonists, thromboxane A2, receptor antagonists, ADP receptor blockers like ticlopidine and clopidogrel, or inhibitors of thromboxane synthase and arachidonic acid metabolism), only the antagonists of platelet receptors have been demonstrated to allow more global interruption of both the initial and final steps of platelet-dependent prothrombotic events. Due to the considerable progress in the development of novel agents aimed to reducing platelet-derived thrombosis, various antiplatelet drugs have been invented, which are rationally based on interrupting specific sites in the sequence of platelet activation, adhesion and aggregation. The antagonists of platelet receptors focus considerable attention, because they are able to directly interfere with the interactions between blood platelets and their ligands. The common feature of these agents is that they are designed to interrupt platelet response at the very initial stage of platelet activation - when the 'outside-in receptor-mediated' triggers signal transduction in platelet cytoplasm. In that sense, the antagonists of platelet receptors are believed to represent quite a new approach to the treatment of platelet thrombosis.

Keywords: antiplatelet drugs, peptidomimetics, monoclonal antibodies, RGD-derived ligands, peptidomimetics