共查询到20条相似文献,搜索用时 31 毫秒
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Thomas C. Warren John J. Miglietta Anthony Shrutkowski Janice M. Rose Sheri L. Rogers Klaus Lubbej Cheng K. Shih Gary O. Caviness Richard Ingraham Deborah E. H. Palladino Eva David Grace C. Chow Elizabeth B. Kopp Kenneth A. Cohen Jan A. Glinski Peter R. Farina Peter M. Grob 《Protein expression and purification》1992,3(6):479-487
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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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J Balzarini M J Pérez-Pérez A San-Félix M J Camarasa I C Bathurst P J Barr E De Clercq 《The Journal of biological chemistry》1992,267(17):11831-11838
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