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Target intelligence / Profile preview
Kallikreins (KLK)
- Target
- KLK
- Molecular classification
- Enzyme, Serine Protease
01
Overview
Kallikreins are a subgroup of serine proteases involved in various physiological processes, including blood pressure regulation, inflammation, and cancer biology. They are divided into plasma kallikrein and tissue kallikrein-related peptidases (KLKs). They function via cleavage of peptide bonds in proteins, most notably high and low molecular weight kininogens to release bradykinin and kallidin. Dysregulation of kallikreins is implicated in hypertension, inflammatory diseases, and cancer, making them attractive therapeutic targets.
- Other names
- Plasma kallikreinTissue kallikrein-related peptidasesKLKsProstate-specific antigenPSAKLK3
02
Mechanism of action
Serine protease inhibition; modulation of bradykinin/kallidin pathways
03
Biological functions
Blood pressure regulationSemen liquefactionSkin desquamationInflammationExtracellular matrix remodelingCell signalingApoptosisAngiogenesisCell proliferationCell migrationCell invasion
04
Disease associations
HypertensionInflammatory diseasesCancerThrombosis
05
Safety considerations
Off-target effects of inhibitorsIncomplete inhibition kineticsDysregulation of kallikrein pathways leading to unintended consequences
06
Interacting drugs
Aprotinin
1 more in the full profile.
07
Biomarkers
Prostate-specific antigen (PSA/KLK3)
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