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A_(8—10)替换的胰岛素类似物的合成及生物活性
引用本文:杨士珍,林威,黄一丁,冯佑民,钮经义.A_(8—10)替换的胰岛素类似物的合成及生物活性[J].生物化学与生物物理学报,1994(6).
作者姓名:杨士珍  林威  黄一丁  冯佑民  钮经义
作者单位:中国科学院上海生物化学研究所
基金项目:中国科学院“八·五”重点科研项目,国家自然科学基金
摘    要:本文报道了用Fmoc固相法合成3种胰岛素A链小环(A8-10)被不同碱性氨基酸取代的A链类似物,并分别与天然胰岛素B链重组成相应胰岛素类似物;经受体结合,整体活性及抗体结合实验,均表现出相应的活性。从中可以推测出:A链小环区域不是胰岛素表现生物活性的重要部位,而是胰岛素与其抗体结合较重要的区域。

关 键 词:A_(8-10)替换  胰岛素类似物  受体结合  抗原性

Synthesis and Activity of Insulin Analogues with Alteration at A_(8-10)
YANG Shi-Zhen,LIN Wei,HUANG Yi-Ding,DENG You-Min and NIU Jing-Yi.Synthesis and Activity of Insulin Analogues with Alteration at A_(8-10)[J].Acta Biochimica et Biophysica Sinica,1994(6).
Authors:YANG Shi-Zhen  LIN Wei  HUANG Yi-Ding  DENG You-Min and NIU Jing-Yi
Abstract:Three insulin A-chain analogues with substitution by basic amino acia residues at A8-10 positions inside the intra-disulfide bonds were synthesized by the solid phase methods with Fmoc protection strategy.The corresponding insulin analogues obtained through reconstitution with the B-chain of porcine insulin showed definite activities in receptor binding,mouse convulsion test and antigenicity assays.It is suggested that this region inside A6-11 was not much concerned with biological activities,but rather more important antigenically in the binding to its antibodies.
Keywords:A8-10 substitutions  Insulin analogues  Receptor binding  Antigenicity  
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