共查询到20条相似文献,搜索用时 31 毫秒
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YADD mutants of human immunodeficiency virus type 1 and Moloney murine leukemia virus reverse transcriptase are resistant to lamivudine triphosphate (3TCTP) in vitro.
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Paul L. Boyer Hong-Qiang Gao Patrick K. Clark Stefan G. Sarafianos Edward Arnold Stephen H. Hughes 《Journal of virology》2001,75(14):6321-6328
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Structures of HIV-1 RT-DNA complexes before and after incorporation of the anti-AIDS drug tenofovir 总被引:3,自引:0,他引:3
Tuske S Sarafianos SG Clark AD Ding J Naeger LK White KL Miller MD Gibbs CS Boyer PL Clark P Wang G Gaffney BL Jones RA Jerina DM Hughes SH Arnold E 《Nature structural & molecular biology》2004,11(5):469-474
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Vivet-Boudou V Paillart JC Burger A Marquet R 《Nucleosides, nucleotides & nucleic acids》2007,26(6-7):743-746
With the emergence of HIV strains resistant or cross-resistant to nearly all antiretroviral regimen, novel therapy approaches have to be considered. As a part of our current work on viral mutagenic compounds, we prepared 1-(2' -deoxy-beta-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide (2' -deoxy-ribavirin) and its 5' -triphosphate derivative. The nucleoside mutagenic activity was evaluated on HIV-1 NL4-3 in CEMx174 cell culture. After 2.5 months, no reduction on HIV-1 viability was observed. On the other hand, in vitro experiments with purified HIV-1 RT demonstrated that the triphosphate analog can be incorporated opposite to several natural nucleosides. 相似文献
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Martin Tremblay Richard C. Bethell Michael G. Cordingley Patrick DeRoy Jianmin Duan Martin Duplessis Paul J. Edwards Anne-Marie Faucher Ted Halmos Clint A. James Cyrille Kuhn Jean-Éric Lacoste Louie Lamorte Steven R. LaPlante Éric Malenfant Joannie Minville Louis Morency Sébastien Morin Claudio F. Sturino 《Bioorganic & medicinal chemistry letters》2013,23(9):2775-2780
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P Franchetti G Abu Sheikha L Cappellacci M Grifantini E Balestra C F Perno G Brandi L Rossi M Magnani 《Nucleosides & nucleotides》1999,18(4-5):989-990
A new antiviral drug with both anti-HSV and anti-HIV activity was synthesized by coupling Acyclovir and the acyclic nucleoside phosphonate (R)PMPA. The heterodinucleotide ACVpPMPA encapsulated into autologous erythrocytes was added to human macrophages providing an effective in vitro protection from HSV-1 and HIV-1 replication. 相似文献
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V. Vivet-Boudou J.-C. Paillart A. Burger R. Marquet 《Nucleosides, nucleotides & nucleic acids》2013,32(6-7):743-746
With the emergence of HIV strains resistant or cross-resistant to nearly all antiretroviral regimen, novel therapy approaches have to be considered. As a part of our current work on viral mutagenic compounds, we prepared 1-(2′ -deoxy-β-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide (2′ -deoxy-ribavirin) and its 5′ -triphosphate derivative. The nucleoside mutagenic activity was evaluated on HIV-1 NL4-3 in CEMx174 cell culture. After 2.5 months, no reduction on HIV-1 viability was observed. On the other hand, in vitro experiments with purified HIV-1 RT demonstrated that the triphosphate analog can be incorporated opposite to several natural nucleosides. 相似文献
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Ambrose Z Boltz V Palmer S Coffin JM Hughes SH Kewalramani VN 《Journal of virology》2004,78(24):13553-13561
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Z Dang K Qian P Ho L Zhu KH Lee L Huang CH Chen 《Bioorganic & medicinal chemistry letters》2012,22(16):5190-5194
Betulinic acid derivatives modified at the C28 position are HIV-1entry inhibitors such as compound A43D; however, modified at the C3 position instead of C28 give HIV-1 maturation inhibitor such as bevirimat. Bevirimat exhibited promising pharmacokinetic profiles in clinical trials, but its effectiveness was compromised by the high baseline drug resistance of HIV-1 variants with polymorphism in the putative drug binding site. In an effort to determine whether the viruses with bevirimat resistant polymorphism also altered their sensitivities to the betulinic acid derivatives that inhibit HIV-1 entry, a series of new betulinic acid entry inhibitors were synthesized and tested for their activities against HIV-1 NL4-3 and NL4-3 variants resistant to bevirimat. The results show that the bevirimat resistant viruses were approximately 5- to10-fold more sensitive to three new glutamine ester derivatives (13, 15 and 38) and A43D in an HIV-1 multi-cycle replication assay. In contrast, the wild type NL4-3 and the bevirimat resistant variants were equally sensitive to the HIV-1 RT inhibitor AZT. In addition, these three new compounds markedly improved microsomal stability compared to A43D. 相似文献