Neidle S, Urpi L, Serafinowski P, Whitby D
Cancer Research Campaign Biomolecular Structure Unit, Institute of Cancer Research, Sutton, Surrey, U.K.
Biochem Biophys Res Commun. 1989 Jun 15;161(2):910-6. doi: 10.1016/0006-291x(89)92685-5.
The crystal structure of the nucleoside 2',3'-dideoxyformycin A has been determined. The structure shows a syn conformation about the glycosidic bond, stabilised by an intramolecular hydrogen bond between the 05' and N3 atoms. HIV activity was examined in a syncytium inhibition assay. In contrast to the marked decrease in viral titre observed with 2',3'-dideoxycytidine, the formycin analogue produced no effect. It may be concluded that the syn conformation for a dideoxy nucleoside is probably deleterious to HIV inhibition of HIV replication.
已确定核苷2'，3'-双脱氧间型霉素A的晶体结构。该结构显示糖苷键呈顺式构象，由05'和N3原子之间的分子内氢键稳定。在合胞体抑制试验中检测了HIV活性。与2'，3'-双脱氧胞苷观察到的病毒滴度显著降低相反，间型霉素类似物没有产生影响。可以得出结论，双脱氧核苷的顺式构象可能不利于HIV对HIV复制的抑制。
