Pardridge W M, Boado R J
Department of Medicine, UCLA School of Medicine 90024-1682.
FEBS Lett. 1991 Aug 19;288(1-2):30-2. doi: 10.1016/0014-5793(91)80996-g.
The cellular uptake of a model antisense oligonucleotide complementary to 21 bases of the bovine GLUT-1 glucose transporter mRNA and a model vasopressin peptide that were biotinylated, was markedly stimulated by the presence of avidin, a cationic protein. Conversely, the bacteria homologue of avidin, streptavidin, which is a slightly acidic protein, did not facilitate cellular uptake. The avidin-mediated uptake of biotinylated derivatives was competitively inhibited by another cationic protein, protamine, with a Ki of 5 micrograms/ml; was saturable, temperature- and time-dependent; and was associated with endocytosis. The use of the avidin-biotin system provides a new approach to increasing the cellular uptake of antisense oligonucleotides or peptides.
与牛GLUT-1葡萄糖转运蛋白mRNA的21个碱基互补的模型反义寡核苷酸以及生物素化的模型血管加压素肽的细胞摄取，受到阳离子蛋白抗生物素蛋白的显著刺激。相反，抗生物素蛋白的细菌同源物链霉抗生物素蛋白是一种微酸性蛋白，它不能促进细胞摄取。抗生物素蛋白介导的生物素化衍生物摄取受到另一种阳离子蛋白鱼精蛋白的竞争性抑制，抑制常数Ki为5微克/毫升；具有饱和性、温度依赖性和时间依赖性；并且与内吞作用有关。抗生物素蛋白-生物素系统的应用为增加反义寡核苷酸或肽的细胞摄取提供了一种新方法。
