蛋白水解酶转肽使猪胰岛素转成人胰岛素

利用赖氨酸专一性的蛋白水解酶进行了酶促人胰岛素半合成反应，猪胰岛素经该酶切去Ｂ链羧基端丙氨酸形成去丙氨酸胰岛素素ＤＡＩ。进一步在水／有机溶剂介质中该酶的转肽反应，使Ｂ链生成苏氨酸叔丁酯羧基末端，水解去酯后产生人胰岛素。研究了转肽反应的最佳条件。转肽反应生成的人胰岛素具有较强的生物活性。

A New Procedure for Semi synthesis of Human Insulin from Porcine Insulin by Transpeptidation with Protease

The semi synthesis of human insulin with lyticus protease which only hydrolyzes acid side peptide bond of lysine is studied.Porcine insulin is transformed into deletion alanine insulin (DAI) by cutting the B chain's acid end amino acid alanine with lyticus protease.Deletion alanine insulin is further changed to thronine tert butyl ester in the B chain's acid end through transpeptidation reaction with the catalysis of lyticus protease.The human insulin is formed after the tert butyl ester hydrolyzed.The most favor conditions for transpeptidation reaction and the biological activities of the product of human insulin are also studied,the results show that the semi synthesis human insulin has fairly high biological activities.