Chapter 8. Anticoagulant Strategies Targeting Thrombin and Factor Xa

摘要: Publisher Summary In recent times, research on novel thrombin inhibitors, the exploration of applications oral inhibitors and development therapeutically useful low molecular weight competitive factor Xa is receiving significant growing attention. This chapter discusses recently described specific small molecule direct in addition to summarizing clinical experiences with inhibitors. Finally, approaches inhibit Xa, enzyme within prothrombinase complex, ultimately responsible for conversion inactive prothrombin procoagulant thrombin. The blood coagulation system involves a variety enzymes (zymogens) into active target existing anti-coagulant drugs. Thrombin, serine protease trypsin-like specificity, plays pivotal role cascade through final fibrinogen fibrin. Thrombin also most potent platelet agonist known and, therefore, positions as central mediator both thrombosis normal hemostasis. major classes compounds that are currently used anti-coagulants all indirectly activity Heparin, its action plasma proteins, anti-thrombin III heparin cofactor II, inhibits other proteases. Side effects, limitations efficacy, bleeding complications these agents have stimulated search novel, more direct, key enzymes.