Kallikrein-1 (KLK1) (KLK1)

Tissue Kallikrein, specifically known as Kallikrein-1 (KLK1), is a secreted serine protease that serves as the primary kinin-generating enzyme in the human body [1.1.3, 1.3.1]. It is a key component of the kallikrein-kinin system, where it cleaves low-molecular-weight kininogen to release kallidin (lysyl-bradykinin), a potent vasodilator [1.2.1, 1.3.3]. This enzymatic activity plays a vital role in regulating blood pressure, maintaining renal function, and modulating inflammatory responses [1.2.1, 1.3.2]. KLK1 is highly expressed in the kidneys, pancreas, and salivary glands, and its downstream signaling through bradykinin B2 receptors promotes the release of nitric oxide and prostacyclin [1.2.1, 1.3.3]. In disease states, reduced levels of KLK1 are associated with hypertension, ischemic stroke, and diabetic nephropathy, making it a target for augmentation therapies [1.3.3, 1.4.3]. Conversely, overactivity of KLK1 in the airways is linked to mucus hypersecretion in asthma, leading to the development of specific inhibitors [1.3.4]. Clinically, human urinary kallikrein is used to treat acute ischemic stroke, while recombinant forms are being investigated for broader cardiovascular and renal applications [1.3.3, 1.2.5].

Other names

Tissue kallikreinhK1Glandular kallikreinKallidinogenasePancreatic/renal kallikreinKidney/pancreas/salivary gland kallikrein

Kallikrein-1 cleaves low-molecular-weight kininogen (LMWK) to release kallidin (lysyl-bradykinin), which subsequently activates bradykinin B2 receptors on endothelial cells, triggering the release of nitric oxide and prostacyclin to induce vasodilation and provide tissue protection [1.2.1, 1.3.3].