Target intelligence / Profile preview

Physiological coagulation and regulatory proteins

Molecular classification
Serine protease, Serine protease inhibitor (Serpin), Glycoprotein, Enzyme cofactor
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Overview

Physiological coagulation and regulatory proteins in human plasma represent a complex system of enzymes, cofactors, and inhibitors that maintain hemostasis by balancing clot formation and dissolution (Palta et al., 2014). This system primarily consists of serine proteases, such as Thrombin (Factor IIa) and Factor Xa, which are activated in a cascading fashion to convert fibrinogen into a stable fibrin clot (Gale, 2011). Regulatory proteins, including Antithrombin III, Protein C, and Protein S, serve as critical checkpoints to prevent excessive thrombosis and ensure blood flow remains fluid (Dahlbäck, 2000). Dysregulation of these proteins leads to significant pathologies, ranging from life-threatening bleeding disorders like Hemophilia to thromboembolic events such as deep vein thrombosis and stroke (StatPearls, 2023). Consequently, these proteins are among the most clinically significant therapeutic targets, with drugs like direct oral anticoagulants (DOACs), heparins, and vitamin K antagonists acting to modulate their activity. Understanding the interplay between these factors is essential for managing cardiovascular health and surgical outcomes.

Other names
Coagulation factorsClotting factorsPlasma proteasesHemostatic proteinsBlood clotting system
02

Mechanism of action

Direct inhibition of Factor Xa; direct inhibition of Thrombin (Factor IIa); potentiation of Antithrombin III; inhibition of Vitamin K epoxide reductase (VKORC1) to prevent synthesis of functional factors II, VII, IX, and X; activation of plasminogen to plasmin for fibrinolysis.

03

Biological functions

HemostasisBlood coagulationFibrinolysisProteolysisWound healing
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Disease associations

Venous thromboembolism (VTE)Deep vein thrombosis (DVT)Pulmonary embolism (PE)StrokeMyocardial infarctionHemophiliaVon Willebrand diseaseDisseminated intravascular coagulation (DIC)
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Safety considerations

Major hemorrhageGastrointestinal bleedingIntracranial hemorrhageHeparin-induced thrombocytopenia (HIT)Drug-drug interactions (e.g., with CYP3A4 or P-gp modulators)
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Interacting drugs

Rivaroxaban

11 more in the full profile.

07

Biomarkers

Prothrombin Time (PT)Activated Partial Thromboplastin Time (aPTT)International Normalized Ratio (INR)D-dimerAnti-Xa levelsFibrinogen levels

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