Hirudisins. Hirudin-derived thrombin inhibitors with disintegrin activity.
نویسندگان
چکیده
منابع مشابه
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...
متن کاملInhibition of Human α-Thrombin with Small Covalent Inhibitors and r-Hirudin
Thrombin is a key serine protease involved in the blood cascade. Two small molecular inhibitors, 4-nitrophenyl diethylphosphate (paraoxon) and 4-nitrophenyl 2-propyl methylphosphonate (MPNP), covalently bond to the active-site Ser to form a mimic of the tetrahedral intermediate found in thrombin-catalyzed reactions. The pH dependence of their inhibition of human α-thrombin at 25.0 + 0.1C was de...
متن کاملCatabolism 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-...
متن کاملStability 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...
متن کاملA strong thrombin-inhibitory prourokinase derivative with sequence elements from hirudin and the human thrombin receptor.
In order to design plasminogen activators with improved thrombolytic properties, bifunctional proteins with both plasminogen-activating and anticoagulative activity were constructed by fusing a thrombin-inhibitory moiety itself comprises four elements: linker 1, a motif directed to thrombin's active site, linker 2 and a fragment of hirudin which binds to the fibrinogen-recognition site of throm...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1992
ISSN: 0021-9258
DOI: 10.1016/s0021-9258(18)35754-5