The aim of this study was to investigate the interaction between polymers polyApolyU (RNA) and two general anti-viral drugs with anti-HIV-1 activities. Tm experiment showed that the compounds had interacted with RNA, ...The aim of this study was to investigate the interaction between polymers polyApolyU (RNA) and two general anti-viral drugs with anti-HIV-1 activities. Tm experiment showed that the compounds had interacted with RNA, and CD spectra also observed the changes of RNA conformation induced by the compounds. Cytometric flow analysis indicated that ribavirin and DII-18-2 could decrease the percentage of hypodiploid cells, especially ribavirin.展开更多
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
人免疫缺陷病毒1(human immunodeficiency virus type 1,HIV-1)蛋白酶活性的严格调控对于病毒的生存至关重要。在病毒蛋白表达及病毒颗粒装配过程中,处于病毒前体蛋白Gag-Pol中的蛋白酶必须以无活性状态存在,避免前体蛋白Gag-Pol和Gag...人免疫缺陷病毒1(human immunodeficiency virus type 1,HIV-1)蛋白酶活性的严格调控对于病毒的生存至关重要。在病毒蛋白表达及病毒颗粒装配过程中,处于病毒前体蛋白Gag-Pol中的蛋白酶必须以无活性状态存在,避免前体蛋白Gag-Pol和Gag被提前酶切加工(前体蛋白早成熟化)。干扰HIV-1蛋白酶活性的调控机制,特异性激活前体蛋白中的蛋白酶,诱导前体蛋白早成熟化,就可直接抑制病毒复制。根据这一设想,利用前期已建立的细胞水平HIV-1前体蛋白早成熟化激活剂筛选模型,对3500个化合物进行筛选与评价,得到6个活性化合物具有激活作用,并具有一定的抗病毒活性,同时在一定程度上诱导了HIV-1感染细胞的凋亡。本研究为抗病毒药物的研发提供了思路。展开更多
基金This project was supported by the National Natural Science Foundation of China Doctoral Program Foundation of China.
文摘The aim of this study was to investigate the interaction between polymers polyApolyU (RNA) and two general anti-viral drugs with anti-HIV-1 activities. Tm experiment showed that the compounds had interacted with RNA, and CD spectra also observed the changes of RNA conformation induced by the compounds. Cytometric flow analysis indicated that ribavirin and DII-18-2 could decrease the percentage of hypodiploid cells, especially ribavirin.
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.
文摘人免疫缺陷病毒1(human immunodeficiency virus type 1,HIV-1)蛋白酶活性的严格调控对于病毒的生存至关重要。在病毒蛋白表达及病毒颗粒装配过程中,处于病毒前体蛋白Gag-Pol中的蛋白酶必须以无活性状态存在,避免前体蛋白Gag-Pol和Gag被提前酶切加工(前体蛋白早成熟化)。干扰HIV-1蛋白酶活性的调控机制,特异性激活前体蛋白中的蛋白酶,诱导前体蛋白早成熟化,就可直接抑制病毒复制。根据这一设想,利用前期已建立的细胞水平HIV-1前体蛋白早成熟化激活剂筛选模型,对3500个化合物进行筛选与评价,得到6个活性化合物具有激活作用,并具有一定的抗病毒活性,同时在一定程度上诱导了HIV-1感染细胞的凋亡。本研究为抗病毒药物的研发提供了思路。
