高受体结合和低免疫原性的［B1—Ala，B2—Ala］－胰岛素

通过化学半合成从天然猪胰岛素得到［Ｂ１－Ａｌａ，Ｂ２－Ａｌａ］胰岛素。这一胰岛素类似物经聚丙烯酰胺凝胶电泳和ＨＰＬＣ鉴定证明是均一的，氨基酸组成与理论值相符生物活性测定结果表明：［Ｂ１－Ａｌａ，Ｂ２－Ａｌａ］－胰岛素的体内活力与天然猪胰岛素相同，而与人胎盘细胞膜胰岛素受体的结合能力为天然猪胰岛素的１３２％。这一结果进一步说明胰岛素Ｂ链Ｎ端肽段参子与受体相互作用。此外，［Ｂ１－Ａｌａ，Ｂ２－Ａｌａ］－胰岛素的免疫活性很低，远小于天然猪胰岛素的４％。

[B1-Ala, B2-Ala]-Insulin:An Insulin Analogue with Higher Receptor Binding Capacity and Lower Immunogenicity

The homogeneousB1-Ala,B2-Ala]-insulin as judged by PAGE and HPLO was prepared by chemical semisynthesis from native porcine insulin.The amino acid composition of this insulin analogue was found to be identical to the theoretical value.The activity in vivo,receptor binding capaeity on human placental membrane and the immunoactivity ofB1-Ala,B2-Ala]-insulin were 100%,132% and much less than 4%,respectively,when compared with those of the native porcine insulin.The effect of the N-terminal peptide sequence of Bchain on the interaction between insulin and insulin receptor has been discussed.