The hirudin-binding site of human α-thrombin
نویسندگان
چکیده
منابع مشابه
Inhibition 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 کاملThe 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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Thrombin is an allosteric serine protease existing in two forms, slow and fast, targeted toward anticoagulant and procoagulant activities. The slow --> fast transition is induced by Na+ binding to a site contained within a cylindrical cavity formed by three antiparallel beta-strands of the B-chain (Met180-Tyr184a, Lys224-Tyr228, and Val213-Gly219) diagonally crossed by the Glu188-Glu192 strand....
متن کاملLocalization of thrombomodulin-binding site within human thrombin.
A binding site for thrombomodulin on human thrombin (alpha-thrombin) was elucidated by identifying an epitope for a monoclonal antibody for thrombin (MT-6) which inhibited the activation of protein C by the thrombin-thrombomodulin complex by directly inhibiting the binding of thrombin to thrombomodulin. An 8.5-kDa fragment isolated by digestion of thrombin with Staphylococcus aureus V8 protease...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1989
ISSN: 0021-9258
DOI: 10.1016/s0021-9258(18)83213-6