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用固相合成和基因定点突变方法 ,分别制备了保留高生物活力的 [A1 3 1 4GABA ,A2 1Ala]猪胰岛素和 [A3Thr]人胰岛素 .结果显示 ,非编码的γ 氨基丁酸能够取代胰岛素中位于A1 3 A1 4位置的二肽Leu Tyr;高度保守且参与受体结合的A3Val可以被亲水的Thr取代 .报道上述 2个胰岛素类似物的单晶体培养和X 射线衍射的初步晶体学研究 .
[A1 3 1 4GABA, A2 1Ala] porcine insulin and [A3Thr] human insulin with high bioactivity were prepared by solid phase synthesis and site-directed mutagenesis, respectively. The results showed that non-coding gamma aminobutyric acid could replace insulin The dipeptide Leu Tyr located at the A1 3 A1 4 position; A3Val, which is highly conserved and involved in receptor binding, can be replaced by hydrophilic Thr.A single crystal culture and X-ray diffraction studies of the above two insulin analogues were reported.