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Human tissue kallikrein (also known as KLK1) is a serine protease enzyme primarily produced in the kidneys, pancreas, and salivary glands[4]. It plays a critical role in the regulation of microcirculation, blood flow, and blood pressure, mainly through the local generation of bioactive peptides including bradykinin, which acts on bradykinin B1 and B2 receptors[3]. In therapeutic contexts, recombinant forms such as DM199 (developed by DiaMedica Therapeutics) are being investigated for the treatment of acute ischemic stroke, chronic kidney disease, and other ischemic-related diseases[2][4]. Natural forms (human urinary kallikrein, HUK/Kailikang) are already approved and widely used in China for acute ischemic stroke, where they have demonstrated improved perfusion and neurological outcomes[5]. KLK1’s mechanism of action involves vasodilation, angiogenesis, and anti-inflammatory effects, primarily via activation of the kallikrein-kinin system[2][3][5].
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