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Tissue kallikreins, human urinary and pancreatic kallikrein, were inhibited by alpha 1-proteinase inhibitor, but the other inhibitors in plasma could not inhibit kallikrein activity towards a synthetic substrate. The kallikrein-inhibitor complex was identified by Sephadex G-150 gel filtration. The inhibition rate of urinary kallikrein by alpha 1-proteinase inhibitor was smaller than that of pancreatic kallikrein, and a less acidic subform of kallikrein was inhibited more rapidly than the more acidic one. Moreover, asialo-kallikrein was inhibited more rapidly than native kallikrein.
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