Abstract
Venous and arterial thromboembolic diseases are still the most frequent causes of death and disability in high-income countries. Clinical anticoagulants are inhibitors of enzymes involved in the coagulation pathway, such as thrombin and factor Xa. Thrombin is a key enzyme of blood coagulation system, activating the platelets, converting the fibrinogen to the fibrin net, and amplifying its self-generation by the activation of factors V, VIII, and XI. Thrombin has long been a target for the development of oral anticoagulants. Furthermore, selective inhibitors of thrombin represent a new class of antithrombotic agents. For these reasons, a number of specific thrombin inhibitors are under evaluation for possible use as antithrombotic drugs. This paper summarizes old and new interests of specific thrombin inhibitors described in different animals.
Highlights
Thrombin is a multifunctional serine proteinase that cleaves substrates after arginine (Arg) or lysine (Lys) residues [1]. This enzyme plays an important role in different biological phenomena, such as hemostasis, thrombosis, inflammation, and proliferative response [2, 3]
Thrombin is the key enzyme of the blood coagulation system, presenting many important biological functions, such as the activation of platelets, conversion of fibrinogen to fibrin, and feedback amplification of coagulation
Amblin is the first thrombin inhibitor isolated from ixodid tick haemolymph of Amblyomma hebraeum. It is composed of 151 amino acids and contains 14 cysteines and two Kunitzlike domains [93]. Another interesting thrombin inhibitor described is boophilin, from the ixodid tick, Rhipicephalus (Boophilus) microplus, which has 12 cysteines distributed in two Kunitz-type domains that interact with thrombin by different manner when compared to that of hirudin or rhodniin [94]
Summary
Thrombin is a multifunctional serine proteinase that cleaves substrates after arginine (Arg) or lysine (Lys) residues [1]. This enzyme plays an important role in different biological phenomena, such as hemostasis, thrombosis, inflammation, and proliferative response [2, 3]. Thrombin is the key enzyme of the blood coagulation system, presenting many important biological functions, such as the activation of platelets, conversion of fibrinogen to fibrin, and feedback amplification of coagulation. The precise generation of thrombin at vascular injury sites is the result of an ordered series of reactions collectively referred to as blood coagulation cascade [4, 5]
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