Target intelligence / Profile preview

Prothrombin (Coagulation factor II) (F2)

Target
F2
Molecular classification
Serine protease, Coagulation factor, Zymogen
01

Overview

Prothrombin (Coagulation factor II) is the inactive zymogen precursor of thrombin, the primary effector of blood coagulation [1]. Pro-exosite I is a discrete binding domain on the prothrombin molecule that serves as the precursor to the anion-binding exosite I found on active thrombin [2]. This site plays a pivotal role in the assembly of the prothrombinase complex, specifically by mediating the interaction between prothrombin and its cofactor, Factor Va [2]. By facilitating this interaction, pro-exosite I ensures the rapid and localized conversion of prothrombin to thrombin at the site of vascular injury [1, 2]. Therapeutic targeting of pro-exosite I, such as with specific DNA aptamers like HD1, aims to inhibit thrombin generation at its source [3, 4]. This approach potentially offers a clinical advantage over direct thrombin inhibitors by providing a more nuanced modulation of the coagulation cascade, potentially reducing the risk of systemic bleeding while maintaining effective antithrombotic activity [2, 3].

Other names
Factor IICoagulation factor IIPro-exosite 1Anion-binding exosite 1 precursor
02

Mechanism of action

Inhibition of the prothrombinase complex assembly by blocking the interaction between prothrombin's pro-exosite I and Factor Va, thereby preventing the conversion of prothrombin to thrombin [2, 3].

03

Biological functions

Blood coagulationHemostasisProthrombinase complex assemblyThrombin generation
04

Disease associations

ThrombosisVenous thromboembolismStrokeMyocardial infarction
05

Safety considerations

Bleeding riskHemorrhageAnticoagulant-induced coagulopathy
06

Interacting drugs

HD1 (Aptamer)

2 more in the full profile.

07

Biomarkers

Prothrombin time (PT)Activated partial thromboplastin time (aPTT)Prothrombin fragment 1.2Thrombin-antithrombin (TAT) complexes

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