Hotoda H, Momota K, Furukawa H, Nakamura T, Kaneko M, Kimura S, Shimada K
Bioscience Research Laboratories, Sankyo Company Ltd., Tokyo, Japan.
Nucleic Acids Symp Ser. 1993(29):59-61.
5'-Modified pentadecadeoxyribonucleotides with a sequence (5'-TGGGAGGTGGGTCTG-3') (15mer) complimentary (antisense) to the tat 2nd splicing acceptor region of human immunodeficiency virus type 1 (HIV-1) were prepared and evaluated for anti-HIV-1 activity. The modified antisense oligodeoxyribonucleotides (AS-ODNs) were synthesized using 5'-modified thymidine 3'-phosphoramidites as the 5'-terminal residues. The structures of the 5'-modified 15mers were confirmed by negative ion LSI mass spectroscopy, and the anti-HIV-1 activities were evaluated in vitro by the MTT assay using MT-4 cells. While the unmodified 15mer had no activity in our assay system, the 15mers bearing modifications with trityl-type substituents at the 5'-end showed high anti-HIV-1 activities.
制备了与人类免疫缺陷病毒1型（HIV-1）tat第2个剪接受体区域序列互补（反义）的（5'-TGGGAGGTGGGTCTG-3'）（15聚体）5'-修饰的十五聚脱氧核糖核苷酸，并对其抗HIV-1活性进行了评估。使用5'-修饰的胸苷3'-亚磷酰胺作为5'-末端残基合成修饰的反义寡脱氧核苷酸（AS-ODN）。通过负离子LSI质谱法确认了5'-修饰的15聚体的结构，并使用MT-4细胞通过MTT测定法在体外评估了抗HIV-1活性。虽然未修饰的15聚体在我们的测定系统中没有活性，但在5'-末端带有三苯甲基型取代基修饰的15聚体显示出高抗HIV-1活性。
