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There are three types of DTIs, dependent on their interaction with the thrombin molecule. Bivalent DTIs (hirudin and analogs) bind both to the active site and exosite 1, while univalent DTIs bind only to the active site. [1] The third class of inhibitors, which are gaining importance recently, is the allosteric inhibitors.
ATC code B01 Antithrombotic agents is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
Heparin cofactor II (HCII), a protein encoded by the SERPIND1 gene, is a coagulation factor that inhibits IIa, and is a cofactor for heparin and dermatan sulfate ("minor antithrombin"). [ 5 ] The product encoded by this gene is a serine protease inhibitor which rapidly inhibits thrombin in the presence of dermatan sulfate or heparin.
The conformational change in AT on heparin-binding mediates its inhibition of factor Xa. For thrombin inhibition, however, thrombin must also bind to the heparin polymer at a site proximal to the pentasaccharide. The highly negative charge density of heparin contributes to its very strong electrostatic interaction with thrombin. [37]
Antithrombin (AT), a serine protease inhibitor, is the major plasma inhibitor of coagulation proteases. [15] LMWHs inhibit the coagulation process by binding to AT via a pentasaccharide sequence. This binding leads to a conformational change of AT, increasing the rate at which it inhibits activated factor X . Once dissociated, the LMWH is free ...
DTIs inhibit thrombin by two ways; bivalent DTIs block simultaneously the active site and exosite 1 and act as competitive inhibitors of fibrin, [13] while univalent DTIs block only the active site and can therefore both inhibit unbound and fibrin-bound thrombin. In contrast, heparin drugs bind in exosite 2 and form a bridge between thrombin ...
Protein C inhibitor is activated by heparin against thrombin. [6] Protein C inhibitor (PCI) is serine protease inhibitor of serpin type that is found in most tissues and fluids, including blood plasma, seminal plasma and urine of human. [7] It is a 52kD glycoprotein and belongs to serine protease inhibitor ( Serpin) super family of protein. [7]
Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor. [3] In 2000, argatroban was licensed by the US Food and Drug Administration (FDA) for prophylaxis or treatment of thrombosis in people with heparin-induced thrombocytopenia (HIT).