用于蛋白质与类胰蛋白酶丝氨酸蛋白酶活性中心可逆偶联的试剂。
Reagents for reversible coupling of proteins to the active centres of trypsin-like serine proteinases.
作者信息
Kalindjian S B, Smith R A
机构信息
Beecham Pharmaceuticals Research Division, Biosciences Research Centre, Surrey, U.K.
出版信息
Biochem J. 1987 Dec 1;248(2):409-13. doi: 10.1042/bj2480409.
Abstract
In order to extend the scope for the application of acyl-enzymes as fibrinolytic agents, p-amidinophenyl ester enzyme substrates were prepared that gave stabilized acyl-enzymes capable of being coupled to other proteins. Coupling was achieved by reaction of protein thiol functions with a 2-pyridyldithio moiety within the acyl group. Acyl-enzymes derived from such substrates were stable enough to permit isolation of reversible conjugates between proteins and the active centres of plasminogen activators. Hydrolytic release of active enzyme from a conjugate of human immunoglobulin G and urokinase could be demonstrated.
摘要
为了扩大酰基酶作为纤溶酶的应用范围，制备了对脒基苯基酯酶底物，该底物能产生可与其他蛋白质偶联的稳定酰基酶。通过蛋白质硫醇官能团与酰基内的2-吡啶二硫部分反应实现偶联。由此类底物衍生的酰基酶足够稳定，能够分离蛋白质与纤溶酶原激活剂活性中心之间的可逆缀合物。可以证明从人免疫球蛋白G与尿激酶的缀合物中水解释放出活性酶。
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