Hirudin is a 7 kDa acidic protein containing 65 amino acid residues that has an isoelectric point of 3.5-4.0. It is not glycosylated and lacks tryptophan, arginine and methionine residues. It is chemically stable between pH 2-12 and at temperatures up to 80°C.
Biochem/physiol Actions
The anticoagulant, hirudin, is the most potent natural inhibitor of both soluble and clot-bound thrombin. It binds thrombin with high affinity, covering more than 20% of its surface area and occluding both the active site and exosite I (fibrinogen and PAR recognition site). Hirudin blocks thrombus growth and platelet activation. It is not metabolized in the bloodstream of humans and is eliminated unchanged via kidney filtration.
The anticoagulant, hirudin, is the most potent natural inhibitor of both soluble and clot-bound thrombin. It forms a high-affinity 1:1 complex with thrombin, occluding both the proteolytic site and exosite I (fibrinogen and PAR recognition site). Hirudin blocks thrombus growth and platelet activation, and has been suggested as the clinically preferred anticoagulant (over heparin and citrate) for its specific mode of action and absence of side effects. It is not metabolized in the bloodstream of humans and is eliminated unchanged via kidney filtration.
Unit Definition
One unit (ATU) will neutralize one NIH unit of thrombin at 37 °C, based on direct comparison to an NIH thrombin reference standard.
Brain : a journal of neurology, 132(Pt 1), 26-36 (2008-09-06)
Proteases such as matrix metalloproteinases (MMPs) and thrombin are implicated in intracerebral haemorrhage (ICH) but their interactions amongst one another and interdependency remain to be defined. The latter is important since proteases acting through different mechanisms to inflict neurotoxicity would
Journal of immunology (Baltimore, Md. : 1950), 196(2), 832-845 (2015-12-18)
Atypical hemolytic uremic syndrome (aHUS) is a thrombotic microangiopathy with severe renal injury secondary to an overactive alternative complement pathway (AP). aHUS episodes are often initiated or recur during inflammation. We investigated gene expression of the surface complement regulatory proteins
Chemical biology & drug design, 89(1), 67-73 (2016-08-03)
Hirudin is clinically an important drug used for the treatment of cardiac diseases, but has never been elucidated for antileishmanial potential. This study was designed to determine the therapeutic utility of hirudin against leishmaniasis. Binding affinities of 28 potent proteinase
The blood coagulation factor XIII (FXIII) plays a critical role in supporting coagulation and fibrinolysis due to both the covalent crosslinking of fibrin polymers, rendering them resistant to plasmin lysis, and the crosslinking of fibrin to proteins of the fibrinolytic
Activated protein C (APC), a protease with anticoagulant and cytoprotective activities, protects neurons and endothelium from ischemic injury. Drotrecogin-alfa activated, a hyperanticoagulant form of human recombinant APC, is currently being studied in patients with ischemic stroke. How changes in APC
Thrombin is an endolytic serine protease that selectively cleaves the Arg–Gly bonds of fibrinogen to form fibrin and release fibrinopeptides A and B.
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