Recombinant hirudin: A specific thrombin inhibiting anticoagulant for hemodialysis

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Stability of Hirudin, a Thrombin-specific Inhibitor

Hirudin is a 65-amino acid polypeptide with three disulfide linkages. It is stable under extreme pH (1.4712.9), high temperature (95 “C), and in the presence of denaturants (6 M guanidinium chloride or 8 M urea). The thrombin inhibitory activity of hirudin remains unaffected even after cleavage of an internal peptide bond ( L y ~ ~ ‘ A s n ~ ~ ) . One condition which effectively and irreversibl...

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The direct thrombin inhibitor hirudin.

This review discusses the pharmacology and clinical applications of hirudin, a bivalent direct thrombin inhibitor (DTI). Besides the current major indication for hirudin--anticoagulation of patients with heparin-induced thrombocytopenia (HIT)--the experience with hirudin in other indications, especially acute coronary syndromes, are briefly presented. Hirudins have been formally studied prior t...

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Catabolism of hirudin and thrombin-hirudin complexes in the rat.

The metabolic fate of the anticoagulant protein, hirudin, and its complex with thrombin are presently unknown. Therefore we have labelled hirudin and human thrombin-hirudin complex with the residualizing label dilactitol-125I-tyramine (*I-DLT) in order to identify their tissue sites of catabolism in the rat. The rapid plasma clearance of hirudin after intravenous injection was unaffected by *I-...

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Persistent thrombin generation in humans during specific thrombin inhibition with hirudin.

BACKGROUND The degree to which antithrombotic drugs suppress thrombin generation is unknown. Because hirudin, unlike antithrombin III, binds intravascular thrombin rapidly and selectively to yield a circulating inactive complex of 3- to 4-hour half-life, we used intravenous hirudin in humans to investigate the course of thrombin generation during and early after anticoagulation with this potent...

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Efficiently Than Recombinant Hirudin

Background Although the indirect thrombin inhibitor heparin and the more potent direct inhibitor hirudin are useful in preventing thrombosis, a substantial opportunity remains for improving the thrombus selectivity of thrombin inhibitors. Methods and Results To explore the effect of targeting an antithrombin to the surface of a clot, we covalently linked recombinant hirudin to the Fab' (or IgG)...

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ژورنال

عنوان ژورنال: Kidney International

سال: 1994

ISSN: 0085-2538

DOI: 10.1038/ki.1994.228