共查询到20条相似文献,搜索用时 31 毫秒
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Eleftherios Michailidis Andrew D. Huber Emily M. Ryan Yee T. Ong Maxwell D. Leslie Kayla B. Matzek Kamalendra Singh Bruno Marchand Ariel N. Hagedorn Karen A. Kirby Lisa C. Rohan Eiichi N. Kodama Hiroaki Mitsuya Michael A. Parniak Stefan G. Sarafianos 《The Journal of biological chemistry》2014,289(35):24533-24548
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Vivet-Boudou V Isel C Sleiman M Smyth R Ben Gaied N Barhoum P Laumond G Bec G Götte M Mak J Aubertin AM Burger A Marquet R 《PloS one》2011,6(11):e27456
The occurrence of resistant viruses to any of the anti-HIV-1 compounds used in the current therapies against AIDS underlies the urge for the development of new drug targets and/or new drugs acting through novel mechanisms. While all anti-HIV-1 nucleoside analogues in clinical use and in clinical trials rely on ribose modifications for activity, we designed nucleosides with a natural deoxyribose moiety and modifications of position 8 of the adenine base. Such modifications might induce a steric clash with helix αH in the thumb domain of the p66 subunit of HIV-1 RT at a distance from the catalytic site, causing delayed chain termination. Eleven new 2'-deoxyadenosine analogues modified on position 8 of the purine base were synthesized and tested in vitro and in cell-based assays. In this paper we demonstrate for the first time that chemical modifications on position 8 of 2'-deoxyadenosine induce delayed chain termination in vitro, and also inhibit DNA synthesis when incorporated in a DNA template strand. Furthermore, one of them had moderate anti-HIV-1 activity in cell-culture. Our results constitute a proof of concept indicating that modification on the base moiety of nucleosides can induce delayed polymerization arrest and inhibit HIV-1 replication. 相似文献
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Langley DR Walsh AW Baldick CJ Eggers BJ Rose RE Levine SM Kapur AJ Colonno RJ Tenney DJ 《Journal of virology》2007,81(8):3992-4001
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The action of 9-beta-D-arabinofuranosyl-2-fluoroadenine (F-ara-A) on DNA synthesis was evaluated both in whole cells and in vitro. 9-beta-D-Arabinofuranosyl-2-fluoroadenine was converted to its 5'-triphosphate 9-beta-D-arabinofuranosyl-2-fluoroadenine 5'-triphosphate (F-ara-ATP) in cells and then incorporated into DNA in a self-limiting manner. More than 94% of the analogue was incorporated into DNA at the 3' termini, indicating a chain termination action. In vitro DNA primer extension experiments further revealed that F-ara-ATP compared with dATP for incorporation into the A site of the extending DNA strand. The incorporation of F-ara-AMP into DNA resulted in termination of DNA strand elongation. Human DNA polymerase alpha incorporated more F-ara-AMP into DNA than polymerase epsilon (proliferating cell nuclear antigen-independent DNA polymerase delta) and was more sensitive to inhibition by F-ara-ATP. On the other hand, DNA polymerase epsilon was able to excise the incorporated F-ara-AMP from DNA in vitro. The incorporation of F-ara-AMP into DNA was linearly correlated both with inhibition of DNA synthesis and with loss of clonogenicity; thus it may be the mechanism of cytotoxicity. 相似文献
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Quantification of the effects on viral DNA synthesis of reverse transcriptase mutations conferring human immunodeficiency virus type 1 resistance to nucleoside analogues
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Bouchonnet F Dam E Mammano F de Soultrait V Henneré G Benech H Clavel F Hance AJ 《Journal of virology》2005,79(2):812-822
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Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of action
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Jochmans D Deval J Kesteleyn B Van Marck H Bettens E De Baere I Dehertogh P Ivens T Van Ginderen M Van Schoubroeck B Ehteshami M Wigerinck P Götte M Hertogs K 《Journal of virology》2006,80(24):12283-12292