Kallistatin

Kallistatin (SERPINA4) is a circulating serpin distinguished by its specific inhibition of tissue kallikrein, the enzyme that releases the vasodilator peptide bradykinin from kininogen. By blocking tissue kallikrein, kallistatin modulates blood pressure, vascular permeability, and inflammation. It also exerts kallikrein-independent biological effects, including anti-angiogenic activity through binding heparin and VEGF, antioxidant actions, and protection against cardiac and renal injury in animal models. Unlike the antitrypsin branch of the family, its reactive center loop is tailored to kallikrein-type substrates. Recombinant kallistatin is used in kallikrein-kinin pathway assays, hypertension and fibrosis research, and preclinical studies of its gene or protein therapeutics.