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The role of the arginine-B22 residue in insulin action

机译:精氨酸-B22残基在胰岛素作用中的作用

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pWe describe the modification of the side chain of the arginine-B22 residue of insulin by the N8N9-(1, 2-dihydroxycyclohex-1,2-ylene) group and by the adipoyl group. These are the first insulin derivatives described that contain a modified arginine residue in an otherwise unaltered molecule. When tested for their ability to lower blood sugar concentration, both modified insulins showed a specific activity indistinguishable from that of insulin. In view of the fact that the substituent groups involved are very bulky and in one case of opposite charge to that of the side chain, the retention of biological activity casts doubt on the idea, previously generally accepted, that the arginine-B22 residue is essential to the activity of the hormone./p
机译:[P>我们描述了N8N9-(1,2-二羟基环己烷-1,2-基烯及Adipoyl基团的胰岛素精氨酸-B22残基的侧链的修饰。这些是描述的第一胰岛素衍生物,其含有在否则不置换的分子中的改性的精氨酸残基。当测试其降低血糖浓度的能力时,修饰的胰岛素均显示出与胰岛素的特异性活动难以区分。鉴于所涉及的取代基团是非常庞大的并且在一个相反的电荷与侧链的电荷相反,生物活性的保留率对此普遍接受的想法令人疑问,即精氨酸-B22残基是必不可少的对激素的活动。

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