Kobayashi M, Takata Y, Ishibashi O, Sasaoka T, Iwasaki T M, Shigeta Y, Inouye K
Biochem Biophys Res Commun. 1986 May 29;137(1):250-7. doi: 10.1016/0006-291x(86)91203-9.
[LeuA3]-insulin, the third mutant insulin, was semisynthesized and was studied for receptor binding and negative cooperative effects. Receptor binding and biological effects of the mutant insulin were 0.3-0.5% of normal, the lowest among three mutant insulins. However, negative cooperative effects of the mutant insulin were almost normal at higher concentration (greater than 10(-6) M). Monoclonal anti-insulin antibody binding studies revealed that carboxyterminal region of B chain was relatively unchanged. These results suggest that N-terminal region of A-chain extending to A3 is important for receptor binding and confirm that A3 does not play an important role for negative cooperativity.
[亮氨酸A3]胰岛素，即第三种突变胰岛素，经半合成后对其受体结合及负协同效应进行了研究。该突变胰岛素的受体结合及生物学效应为正常水平的0.3 - 0.5%，是三种突变胰岛素中最低的。然而，在较高浓度（大于10⁻⁶ M）时，该突变胰岛素的负协同效应几乎正常。单克隆抗胰岛素抗体结合研究表明，B链的羧基末端区域相对未发生变化。这些结果表明，延伸至A3的A链N端区域对受体结合很重要，并证实A3对负协同性不起重要作用。
