Rose K, Rees A R, Drake C S, Offord R E
Biochem J. 1981 Jun 1;195(3):765-8. doi: 10.1042/bj1950765.
We 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.
我们描述了通过N8N9-(1,2-二羟基环己-1,2-亚基)基团和己二酰基团对胰岛素的精氨酸-B22残基侧链进行的修饰。这些是首次描述的在其他部分未改变的分子中含有修饰精氨酸残基的胰岛素衍生物。当测试它们降低血糖浓度的能力时，两种修饰胰岛素的比活性与胰岛素的比活性没有区别。鉴于所涉及的取代基非常庞大，且在一种情况下与侧链电荷相反，生物活性的保留对先前普遍接受的精氨酸-B22残基对激素活性至关重要这一观点提出了质疑。
