Thrombin Receptor Modulators: Medicinal Chemistry, Biological Evaluation, and Clinical Application

摘要: The serine protease a-thrombin maintains haemostasis through its coagulant, anticoagulant, and platelet-activator functions. This enzyme also has important cellular effects involving cell proliferation, cytokine growth factor release, tissue remodeling, which are mediated by G-protein coupled receptors known as protease-activated (PARs). Thrombin can activate three of the four PAR family members, PAR1 is primary thrombin-responsive receptor in human cells. plays an role during response to injury associated inflammatory processes. blockade offers a new approach for treating various disorders that depend on thrombin generation, including thrombosis restenosis. Antagonists will interrupt thrombin’s function, but not proteolytic activity, thereby providing alternative means attenuate pathological thrombin. chapter deals with topic PAR1, key medicinal chemistry, pharmacology, clinical aspects antagonists, PAR4. full potential antagonists yet be realized commercially, promise novel therapeutics reflected two antiplatelet advanced trials.