[Mechanisms of platelet activation and development of antiplatelet agents].
Platelets are activated by contact with vascular lesions in high flow arteries and are involved in the development of thrombosis, atherosclerosis and the complications of transluminal angioplasty. Hence platelets are one the targets of pharmacological intervention in the prevention and treatment of arterial thrombosis. Understanding of the mechanisms of activation of platelet has enabled the development of new antiplatelet agents and the improvement of their therapeutic usage. The most recent clinical drugs and those currently under development belong to two main families: antagonists of the membrane receptors of activation coupled to signal transducting G proteins which fix circulating stimuli such as ADP, thrombin and TXA2 and inhibitors of the binding of adhesive proteins such as fibrinogen to the GPIIb-IIIa integrin or of von Willebrand factor to the leucine-rich glycoprotein complex GPIb-V-IX.
Cazenave
J P
JP
INSERM U 311, Strasbourg.
Gachet
C
C
Lanza
F
F
D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D019204:GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D015539:Platelet Activation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors; D019038:Platelet Glycoprotein GPIb-IX Complex / Q000037:antagonists & inhibitors; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors; D018179:Receptors, Thrombin / Q000737:chemistry; D015398:Signal Transduction; D013927:Thrombosis / Q000188:drug therapy* / Q000503:physiopathology
D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D019038:Platelet Glycoprotein GPIb-IX Complex; D010980:Platelet Membrane Glycoproteins; D018179:Receptors, Thrombin; D019204:GTP-Binding Proteins
Mécanismes de l'activation plaquettaire et développement de médicaments antiplaquettaires.