Porcine pancreatic kallikrein (KLK1) (KLK1)

Porcine pancreatic kallikrein, also known as kallidinogenase, is a serine protease (EC 3.4.21.35) primarily extracted from the porcine pancreas [UniProt P00755, PubChem CID 10955241]. It acts as a kininogenase, catalyzing the release of kallidin (lysyl-bradykinin) from low-molecular-weight kininogen [UniProt P00755, DrugBank DB09214]. This enzymatic activity is central to the kallikrein-kinin system, which regulates blood pressure, vascular permeability, and inflammatory responses [DrugBank DB09214, PMID: 15671594]. Clinically, it is employed as a vasodilator to improve microcirculation in conditions such as hypertension, peripheral vascular disease, and diabetic complications like retinopathy and nephropathy [DrugBank DB09214, PMID: 15671594]. As a porcine-derived protein, it may trigger hypersensitivity or anaphylactic reactions in sensitive individuals [DrugBank DB09214, PubChem CID 10955241]. Its activity can be inhibited by broad-spectrum serine protease inhibitors such as aprotinin, which are used to manage conditions involving excessive kinin production [UniProt P00755]. This target is significant in both cardiovascular pharmacology and the management of chronic microvascular damage.

Other names

KallidinogenaseGlandular kallikreinKininogenasePancreatic kallikreinKallikrein 1

Porcine pancreatic kallikrein (kallidinogenase) acts by enzymatically cleaving kininogen to release kallidin (lysyl-bradykinin). Kallidin subsequently binds to and activates bradykinin B1 and B2 receptors, triggering the release of secondary messengers like nitric oxide and prostaglandins. This cascade results in potent vasodilation, increased vascular permeability, and improved microcirculation, which helps lower blood pressure and enhance tissue perfusion [DrugBank DB09214, PMID: 15671594].