Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However,...Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.展开更多
目的:研究微小RNA(microRNA,miR)-218-5p靶向调控三磷酸腺苷结合盒超家族G家族第2个成员(ATP-binding cassette sub-family G member 2,ABCG2)基因对Tca-8113细胞的增殖、迁移和侵袭的影响,并探讨其机制。方法:运用实时荧光定量聚合酶...目的:研究微小RNA(microRNA,miR)-218-5p靶向调控三磷酸腺苷结合盒超家族G家族第2个成员(ATP-binding cassette sub-family G member 2,ABCG2)基因对Tca-8113细胞的增殖、迁移和侵袭的影响,并探讨其机制。方法:运用实时荧光定量聚合酶链反应(quantitative Real-time PCR,qRT-PCR)与Western blot检测Tca-8113细胞和NOK细胞中miR-218-5p和ABCG2的表达。通过双荧光素酶报告基因实验检测miR-218-5p和ABCG2靶向关系。用脂质体法将miR-218-5p mimic、ABCG2小干扰RNA(interfering RNA,siRNA)、miR-218-5p mimic+pcDNA-ABCG2分别转染至Tca-8113细胞中,噻唑蓝(methyl thiazol tetrazolium,MTT)法、Transwell法检测Tca-8113细胞的增殖、迁移和侵袭。结果:与NOK细胞比较,Tca-8113细胞miR-218-5p呈显著低表达,ABCG2呈显著高表达(P<0.05)。过表达miR-218-5p、抑制ABCG2均可抑制Tca-8113细胞的增殖和迁移(P<0.05)。双荧光素酶报告基因实验证实miR-218-5p与ABCG2的靶向结合关系。过表达ABCG2可逆转上调miR-218-5p对Tca-8113细胞增殖、迁移和侵袭的抑制作用。结论:上调miR-218-5p的表达可靶向调控ABCG2,抑制Tca-8113细胞的增殖、迁移和侵袭,将可为口腔鳞状细胞癌的治疗提供新的靶点。展开更多
文摘Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.
