Geiger R, Geisen K, Summ H D, Langer D
Hoppe Seylers Z Physiol Chem. 1975 Oct;356(10):1635-49. doi: 10.1515/bchm2.1975.356.2.1635.
Starting from porcine insulin, A1-glycine was substituted by D-alanine and by L-alanine for comparison. Replacement of A1-glycine by L-alanine revealed the known decrease in the biological activity. [A1-D-Alanine]insulin, however, has the same blood sugar lowering activity as insulin and is slightly more active in its influence on the glucose uptake into the rat diaphragm. The specific binding to insulin receptors of rat liver is decreased as, compared to insulin, but increased as compared to the L-alanine analogue.
从猪胰岛素开始,将A1位的甘氨酸分别用D-丙氨酸和L-丙氨酸替代以作比较。用L-丙氨酸替代A1位的甘氨酸会导致生物学活性如已知的那样降低。然而,[A1-D-丙氨酸]胰岛素具有与胰岛素相同的降血糖活性,并且在对大鼠膈肌葡萄糖摄取的影响方面活性略高。与胰岛素相比,其与大鼠肝脏胰岛素受体的特异性结合减少,但与L-丙氨酸类似物相比则增加。