The hexacosapeptide corresponding to the entire amino acid sequence of human α2-plasmin inhibitor fragment T-11 was synthesized by a conventional solution method. Three newly synthesized fragments were combined successively with the protected C-terminal hexadecapeptide ester previously obtained by using the dicyclohexylcarbodiimide-N-hydroxybenzotriazole and azide procedures to afford the protected hexacosapeptide ester. The trifluoromethanesulfonic acid-thioanisole-trifluoroacetic acid procedure was employed to remove all protecting groups of the protected peptide ester at the final stage. The dissociation constant for the interaction between the synthetic α2-plasmin inhibitor fragment T-11 and plasmin was equal to that of the native T-11 from human α2-plasmin inhibitor.
用常规的溶液法合成了对应于人α2-纤溶酶
抑制剂T-11片段全部
氨基酸序列的六十六肽。先后将三个新合成的片段与预先用二环己基碳二
亚胺-N-
羟基苯并三唑和
叠氮化物法制备得到的被保护的C端十六肽酯组合在一起,得到了被保护的六十六肽酯。在最终阶段用
三氟甲磺酸-
噻吩-
三氟乙酸法去除被保护的肽酯的所有保护基团。合成的人α2-纤溶酶
抑制剂T-11片段与纤溶酶相互作用的解离常数,等于天然的人α2-纤溶酶
抑制剂中的T-11片段的解离常数。