Vlasov G P, Izvarina N L, Illarionova N G
Biokhimiia. 1981 May;46(5):942-50.
An intramolecular modification of insulin at the alpha-amino group of glycine (A1) and the epsilon-amino group of lysine (B29) was carried out. The modification resulted in a slight alteration of the insulin secondary structure; the modified hormone possessed a biological activity which was practically identical to that of the natural hormone. Therefore the modified insulin can be used as a high molecular weight physiologically active radical inducer for the synthesis of (A1-B29) polyvinylimidazole derivatives. The molecular weight of the covalently linked polymer can be variable. It was shown that the increase in the amount of modifying polymer in the conjugate results in stabilization of the insulin secondary structure concomitant with a decrease of the biological activity and, moreover, of the immunoresponsiveness of the hormone.
对胰岛素中甘氨酸的α-氨基(A1)和赖氨酸的ε-氨基(B29)进行了分子内修饰。修饰导致胰岛素二级结构略有改变;修饰后的激素具有与天然激素几乎相同的生物活性。因此,修饰后的胰岛素可用作高分子量生理活性自由基诱导剂,用于合成(A1-B29)聚乙烯基咪唑衍生物。共价连接的聚合物的分子量可以是可变的。结果表明,缀合物中修饰聚合物量的增加会导致胰岛素二级结构的稳定,同时生物活性以及激素的免疫反应性降低。