Target intelligence / Profile preview

Plasma Kallikrein (KLKB1)

Target
KLKB1
Molecular classification
Serine Protease, Enzyme
01

Overview

Plasma kallikrein is a serine protease that plays a critical role in blood coagulation, fibrinolysis, and the kinin system. It is produced from prekallikrein by factor XIIa. Plasma kallikrein cleaves high-molecular-weight kininogen (HMWK) to release bradykinin, a potent vasodilator and mediator of inflammation. As a therapeutic target, inhibiting plasma kallikrein can reduce bradykinin production, which is beneficial in treating angioedema and other inflammatory conditions. Conversely, enhancing its activity could promote fibrinolysis and prevent thrombosis, but with potential bleeding risks.

Other names
PrekallikreinFletcher factor
02

Mechanism of action

Inhibition of serine protease activity, preventing cleavage of HMWK and subsequent bradykinin release; disruption of contact activation pathway.

03

Biological functions

Blood coagulationFibrinolysisKinin generationInflammation modulationVasodilation
04

Disease associations

Cardiovascular diseaseInflammationHypertensionAngioedemaThrombosis
05

Safety considerations

Potential for bleeding complications if inhibiting coagulation too stronglyRisk of hypotension due to bradykinin inhibition or altered kinin regulationParadoxical thrombosis under certain conditions
06

Biomarkers

Prekallikrein levels (diagnostic for deficiency)Bradykinin levels (monitoring kinin system activation)

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