Serveau C, Moreau T, Zhou G X, ElMoujahed A, Chao J, Gauthier F
Laboratoire d'Enzymologie et Chimie des Protéines, URA CNRS1334, Université François Rabelais, Tours, France.
FEBS Lett. 1992 Sep 14;309(3):405-8. doi: 10.1016/0014-5793(92)80817-z.
The regulation of tissue kallikrein activity by plasma serine proteinase inhibitors (serpins) was investigated by measuring the association rate constants of six tissue-kallikrein family members isolated from the rat submandibular gland, with rat kallikrein-binding protein (rKBP) and alpha 1-proteinase inhibitor (alpha 1-PI). Both these serpins inhibited kallikreins rK2, rK7, rK8, rK9 and rK10 with association rate constants in the 10(3)-10(4) M-1.s-1 range, whereas only 'true' tissue kallikrein rK1 was not susceptible to alpha 1-PI. This results in slow inhibition of rK1 by plasma serpins, which could explain why this kallikrein is the only member of the gene family identified so far that induces a transient decrease in blood pressure when injected in minute amounts into the circulation.
通过测量从大鼠颌下腺分离出的六个组织激肽释放酶家族成员与大鼠激肽释放酶结合蛋白（rKBP）和α1-蛋白酶抑制剂（α1-PI）的缔合速率常数，研究了血浆丝氨酸蛋白酶抑制剂（丝氨酸蛋白酶抑制剂）对组织激肽释放酶活性的调节作用。这两种丝氨酸蛋白酶抑制剂均以10（3）-10（4）M-1.s-1范围内的缔合速率常数抑制激肽释放酶rK2、rK7、rK8、rK9和rK10，而只有“真正的”组织激肽释放酶rK1对α1-PI不敏感。这导致血浆丝氨酸蛋白酶抑制剂对rK1的抑制作用缓慢，这可以解释为什么这种激肽释放酶是迄今为止鉴定出的基因家族中唯一在微量注入循环系统时会引起血压短暂下降的成员。
