Hassall C H, Johnson W H, Kennedy A J, Roberts N A
FEBS Lett. 1985 Apr 22;183(2):201-5. doi: 10.1016/0014-5793(85)80776-6.
Studies of the inhibition of elastases at a molecular level have resulted in the identification of protected dipeptides which are reversible and highly specific inhibitors of human leucocyte elastase (HLE). These have been further developed by increasing their hydrophilicity and potency to give a new family of elastase inhibitors, typically N alpha-(1-adamantanesulphonyl)-N epsilon-(4-carboxybenzoyl)-L-lysyl-L-alanyl-L-valinal. These compounds are active in pharmacological models designed to detect compounds of potential therapeutic value in the treatment of emphysema.
在分子水平上对弹性蛋白酶抑制作用的研究已鉴定出受保护的二肽，它们是人类白细胞弹性蛋白酶（HLE）的可逆且高度特异性抑制剂。通过增加其亲水性和效力，对这些二肽进行了进一步开发，从而得到了一个新的弹性蛋白酶抑制剂家族，典型的如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。这些化合物在旨在检测对肺气肿治疗具有潜在治疗价值的化合物的药理模型中具有活性。
