Boudier C, Bieth J G
INSERM Unité 237, Université Louis Pasteur de Strasbourg, Faculté de Pharmacie, Illkirch, France.
Biochim Biophys Acta. 1989 Mar 16;995(1):36-41. doi: 10.1016/0167-4838(89)90230-6.
Human mucus proteinase inhibitor is a fast-acting inhibitor of human leucocyte elastase (EC 3.4.21.37) and forms a stable, complex with this enzyme. At physiological ionic strength and temperature and in the presence of 10 mg/ml albumin, the kinetic constants characterizing the interaction between elastase and the non-degraded inhibitor are: kass = 6.4.10(6) M-1.s-1, kdiss = 2.3.10(-3) s-1, Ki = 3.10(-10) M. The partially degraded inhibitor isolated by chymotrypsin-Sepharose chromatography inhibits elastase with similar efficiency, suggesting that if partial proteolysis of the inhibitor occurs in vivo, the latter may still act as a potent antielastase. Mucus proteinase inhibitor therefore plays a physiological antielastase function in upper respiratory tract secretions, since it inhibits elastase with a delay time of 150 ms and behaves like an irreversible inhibitor.
人黏液蛋白酶抑制剂是一种对人白细胞弹性蛋白酶(EC 3.4.21.37)起效迅速的抑制剂,并与该酶形成稳定的复合物。在生理离子强度、温度以及存在10毫克/毫升白蛋白的情况下,表征弹性蛋白酶与未降解抑制剂之间相互作用的动力学常数为:结合常数kass = 6.4×10⁶ M⁻¹·s⁻¹,解离常数kdiss = 2.3×10⁻³ s⁻¹,抑制常数Ki = 3×10⁻¹⁰ M。通过胰凝乳蛋白酶-琼脂糖凝胶色谱法分离得到的部分降解抑制剂对弹性蛋白酶的抑制效率相似,这表明如果抑制剂在体内发生部分蛋白水解,后者仍可能作为一种有效的抗弹性蛋白酶发挥作用。因此,黏液蛋白酶抑制剂在上呼吸道分泌物中发挥着生理抗弹性蛋白酶功能,因为它抑制弹性蛋白酶的延迟时间为150毫秒,且表现得像一种不可逆抑制剂。