Hirudin
From Proteopedia
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| - | <StructureSection load='4htc' size='350' side='right' caption='Hirudin (wheat) complex with thrombin small subunit (aqua) and large subunit (red) (PDB entry [[ | + | <StructureSection load='4htc' size='350' side='right' caption='Hirudin (wheat) complex with glycosylated thrombin small subunit (aqua) and large subunit (red) (PDB entry [[4htc]])' scene=''> |
== Function == | == Function == | ||
[[Hirudin]] (Hir) is a powerful anticoagulant which is found in the leech salivary glands. It is an inhibitor of thrombin (Thr) which converts [[Fibrinogen|fibrinogen]] to [[Fibrin|fibrin]] upon blood clotting<ref>PMID:9579630</ref>. 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]]. | [[Hirudin]] (Hir) is a powerful anticoagulant which is found in the leech salivary glands. It is an inhibitor of thrombin (Thr) which converts [[Fibrinogen|fibrinogen]] to [[Fibrin|fibrin]] upon blood clotting<ref>PMID:9579630</ref>. 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]]. | ||
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== Relevance == | == Relevance == | ||
Hirudin is an effective local treatment in patients with mild to moderate bruises<ref>PMID:11863317</ref>. Hirudin was approved as treatment of heparin-induced thrombocytopenia and unstable angina<ref>PMID:8198374</ref>. | Hirudin is an effective local treatment in patients with mild to moderate bruises<ref>PMID:11863317</ref>. Hirudin was approved as treatment of heparin-induced thrombocytopenia and unstable angina<ref>PMID:8198374</ref>. | ||
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| + | == Structural highlights == | ||
| + | The N-terminal tripeptide of hirudin binds to the heavy chain of thrombin and interacts with two of its active site residues: Ser195 and His57<ref>PMID:1920434</ref>. | ||
</StructureSection> | </StructureSection> | ||
== 3D Structures of Hirudin == | == 3D Structures of Hirudin == | ||
Revision as of 09:53, 22 March 2016
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3D Structures of Hirudin
Updated on 22-March-2016
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
