Hirudin
From Proteopedia
FunctionHirudin (Hir) is a powerful anticoagulant which is found in the leech salivary glands. It is an inhibitor of thrombin (Thr) which converts fibrinogen to fibrin upon blood clotting[1]. Thrombin is produced upon enzymatic cleavage of prothrombin (ProThr). Hirugen (Hirg) is a dodecapeptide of the C-terminal of Hir (sequence NDGDFEEIPEEYL). For additional details see Sean Swale/Human Thrombin Inhibitor and Thrombin. RelevanceHirudin is an effective local treatment in patients with mild to moderate bruises[2]. Hirudin was approved as treatment of heparin-induced thrombocytopenia and unstable angina[3]. Structural highlightsThe N-terminal tripeptide of hirudin (green) binds to the heavy chain of thrombin (magenta) and interacts with two of its active site residues: Ser195 and His57[4]. 3D Structures of Hirudin
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References
- ↑ Fenton JW 2nd, Ofosu FA, Brezniak DV, Hassouna HI. Thrombin and antithrombotics. Semin Thromb Hemost. 1998;24(2):87-91. PMID:9579630 doi:http://dx.doi.org/10.1055/s-2007-995828
- ↑ Stamenova PK, Marchetti T, Simeonov I. Efficacy and safety of topical hirudin (Hirudex): a double-blind, placebo-controlled study. Eur Rev Med Pharmacol Sci. 2001 Mar-Apr;5(2):37-42. PMID:11863317
- ↑ Johnson PH. Hirudin: clinical potential of a thrombin inhibitor. Annu Rev Med. 1994;45:165-77. PMID:8198374 doi:http://dx.doi.org/10.1146/annurev.med.45.1.165
- ↑ Rydel TJ, Tulinsky A, Bode W, Huber R. Refined structure of the hirudin-thrombin complex. J Mol Biol. 1991 Sep 20;221(2):583-601. PMID:1920434
