Target intelligence / Profile preview

Antithrombin III (None)

Target
None
Molecular classification
Glycoprotein, Serpin family, Serine protease inhibitor
01

Overview

Antithrombin III (AT III), also known simply as antithrombin or AT, is a plasma glycoprotein and a member of the serpin (serine protease inhibitor) superfamily. It plays a critical role in regulating blood coagulation by inhibiting several enzymes in the coagulation cascade. Its inhibitory activity is significantly enhanced by heparin; thus, heparin’s anticoagulant effect depends on sufficient levels of functional antithrombin. Deficiency or dysfunction leads to increased risk for venous thromboembolism and related complications.

Other names
AntithrombinATIIISerpin C1SERPINC1 gene product
02

Mechanism of action

Antithrombin III neutralizes target serine proteases by forming an irreversible covalent complex with them. The interaction involves the active site serine residue on thrombin or other target proteases binding to an arginine residue within AT’s reactive center loop. This results in rapid inhibition of clotting enzyme activity—especially when catalyzed by heparin.

03

Biological functions

Regulation of blood coagulationInhibition of thrombinInhibition of coagulation factors IXa, Xa, XIa, XIIa, plasmin, matriptase-3/TMPRSS7Inhibition of serine proteases
04

Disease associations

Venous thromboembolism (VTE)Deep vein thrombosis (DVT)Pulmonary embolism (PE)Hereditary antithrombin deficiencyAcquired antithrombin deficiency (liver disease, nephrotic syndrome, DIC)Thrombosis
05

Safety considerations

DizzinessChest discomfortNauseaDysgeusia (altered taste)CrampsMajor bleeding (rare, especially when combined with heparins)Potential for immunogenicity
06

Interacting drugs

Heparin

1 more in the full profile.

07

Biomarkers

Antithrombin III plasma concentrationAntithrombin III activity

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