Tissue kallikrein-1 (KLK1)

Tissue kallikrein-1 (KLK1) is a member of the serine protease family and a key component of the tissue kallikrein-kinin system. Its primary biological function is the proteolytic cleavage of low-molecular-weight kininogen (LMWK) to release kallidin (lysyl-bradykinin), which subsequently acts on bradykinin receptors to mediate vasodilation, increase vascular permeability, and regulate local blood flow (UniProt P06870). KLK1 is widely expressed in tissues such as the kidney, pancreas, and salivary glands, playing a vital role in maintaining cardiovascular homeostasis and renal function (NCBI Gene 3816). In a clinical context, KLK1 is a therapeutic target for conditions characterized by impaired microcirculation, including ischemic stroke, hypertension, and diabetic complications (PubMed 21504353). Exogenous administration of KLK1, often referred to as kallidinogenase, is utilized to enhance blood flow and provide neuroprotective effects in certain regions (DrugBank DB09074). However, pharmacological intervention must be managed carefully to avoid excessive hypotension or allergic reactions resulting from kinin overproduction.

Other names

Kallikrein-1Glandular kallikreinhK1Kidney kallikreinPancreatic kallikreinUrinary kallikrein

Tissue kallikrein-1 acts by proteolytically cleaving low-molecular-weight kininogen (LMWK) to produce kallidin (lysyl-bradykinin). Kallidin subsequently activates bradykinin B2 receptors, triggering the release of nitric oxide and prostaglandins, which results in vasodilation, increased vascular permeability, and improved microcirculation (UniProt P06870, PubMed 21504353).