Reactome | Factor IIa inhibitors (peptide) binds IIa

Factor IIa inhibitors (peptide) binds IIa

Stable Identifier

R-HSA-9603302

Type

Reaction [binding]

Species

Homo sapiens

Compartment

extracellular region

ReviewStatus

5/5

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Factor IIa inhibitors (peptide) binds IIa

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In the blood coagulation process, prothrombin is proteolytically cleaved to form thrombin (factor IIa) which in turn, acts as a serine protease that converts soluble fibrinogen into insoluble strands of fibrin. Specifically, thrombin converts factor XI to XIa, factor VIII to VIIIa, factor V to Va, fibrinogen to fibrin, and factor XIII to XIIIa. Direct thrombin inhibitors (DTIs) represent a new class of promising anticoagulation agents. DTIs are increasingly being used instead of heparin to provide initial, rapid anticoagulation. Unlike heparin, which requires a mediator (antithrombin) to potentiate anticoagulation, Peptide DTIs can inhibit free and bound thrombin directly. Lepirudin (brand name Refludan) is a recombinant hirudin derived from yeast cells (Weitz et al. 1990). Hirudin is a naturally occurring anticoagulant produced by the salivary glands of medicinal leeches. Bivalirudin (brand name Angiomax, Angiox) is a synthetic analog of hirudin, with a shorter period of binding to thrombin (Gladwell 2002). Desirudin (brand name Iprivask) is another recombinant hirudin derivative that directly inhibits free and fibrin-bound thrombin (Graetz et al. 2011).

Literature References

PubMed ID	Title	Journal	Year
11833835	Bivalirudin: a direct thrombin inhibitor Gladwell, TD	Clin Ther	2002
21932952	Desirudin: a review of the pharmacology and clinical application for the prevention of deep vein thrombosis Avidan, MS, Smith, JR, Tellor, BR, Graetz, TJ	Expert Rev Cardiovasc Ther	2011
2384594	Clot-bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin III-independent inhibitors Massel, D, Hirsh, J, Maraganore, J, Hudoba, M, Weitz, JI	J. Clin. Invest.	1990