Kennedy A J, Cline A, Ney U M, Johnson W H, Roberts N A
Department of Biology, Roche Products Ltd, Welwyn Garden City, U.K.
Eur J Respir Dis. 1987 Nov;71(5):472-8.
The peptide aldehyde Ro 31-3537, N alpha-(1-adamantanesulphonyl)-N epsilon-(4-carboxybenzoyl)-L-lysyl-L-alanyl-L- valinal, is a reversible competitive, hydrophilic, specific inhibitor of elastase. Its Ki against human leucocyte elastase is 6 x 10(-8) M. The effect of this compound has been studied on a model of emphysema in the hamster induced by multiple sequential intratracheal doses of human leucocyte elastase. Concomitant intratracheal dosing of 200 micrograms of inhibitor with the enzyme significantly reduces lung damage as measured by quasi-static lung compliance and by histological assessment of the emphysema.
肽醛Ro 31-3537，Nα-（1-金刚烷磺酰基）-Nε-（4-羧基苯甲酰基）-L-赖氨酰-L-丙氨酰-L-缬氨醛，是一种可逆竞争性、亲水性、弹性蛋白酶特异性抑制剂。其对人白细胞弹性蛋白酶的Ki为6×10⁻⁸M。已在仓鼠中通过多次气管内注射人白细胞弹性蛋白酶诱导的肺气肿模型上研究了该化合物的作用。与酶同时进行气管内给药200微克抑制剂，通过准静态肺顺应性和肺气肿的组织学评估测量，可显著减少肺损伤。
