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Direct thrombin inhibitors (DTIs) are a class of anticoagulant drugs that can be used to prevent and treat embolisms and blood clots caused by various diseases. They inhibit thrombin, a serine protease which affects the coagulation cascade in many ways. DTIs have undergone rapid development since the 90's.
Thrombin is produced by the enzymatic cleavage of two sites on prothrombin by activated Factor X (Xa). The activity of factor Xa is greatly enhanced by binding to activated Factor V (Va), termed the prothrombinase complex. Prothrombin is produced in the liver and is co-translationally modified in a vitamin K -dependent reaction that converts 10 ...
Blood coagulation pathways in vivo showing the central role played by thrombin. Health. Beneficial. Coagulation, also known as clotting, is the process by which blood changes from a liquid to a gel, forming a blood clot. It results in hemostasis, the cessation of blood loss from a damaged vessel, followed by repair.
Coagulation factor X (EC 3.4.21.6), or Stuart factor, is an enzyme of the coagulation cascade, encoded in humans by F10 gene. [5] It is a serine endopeptidase (protease group S1, PA clan ). Factor X is synthesized in the liver and requires vitamin K for its synthesis.
Specifically, antiplatelet drugs inhibit platelet aggregation (clumping together), whereas anticoagulants inhibit specific pathways of the coagulation cascade, which happens after the initial platelet aggregation but before the formation of fibrin and stable aggregated platelet products. [11] [12] Common anticoagulants include warfarin and heparin.
The complex assembles on negatively charged phospholipid membranes in the presence of calcium ions. The prothrombinase complex catalyzes the conversion of prothrombin (factor II), an inactive zymogen, to thrombin (factor IIa), an active serine protease. The activation of thrombin is a critical reaction in the coagulation cascade, which ...
Heparin, also known as unfractionated heparin (UFH), is a medication and naturally occurring glycosaminoglycan. [ 3 ][ 4 ] Heparin is a blood anticoagulant that increases the activity of antithrombin. [ 5 ] It is used in the treatment of heart attacks and unstable angina. [ 3 ]
Protein C, also known as autoprothrombin IIA and blood coagulation factor XIV, [5]: 6822 [6] is a zymogen, that is, an inactive enzyme. The activated form plays an important role in regulating anticoagulation , inflammation , and cell death and maintaining the permeability of blood vessel walls in humans and other animals.