排序方式: 共有21条查询结果,搜索用时 15 毫秒
1.
Kelvin K. Ogilvie H. R. Hanna Nghe Nguyen-ba Kendall O. Smith 《Nucleosides, nucleotides & nucleic acids》2013,32(4):507-513
Abstract N-Substituted Glyceropurines have been prepared. The N-dimethylaminomethyleneated and N-acetylated glyceroguanine derivatives have significant activity against Herpesviruses. 相似文献
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Paul Nguyen-Ba Nola Lee Helen Mitchell Laval Chan Miguel Quimpère 《Bioorganic & medicinal chemistry letters》1998,8(24):3675-3560
A novel class of cyclic nucleotide analogs has shown anti-HCMV activity. The synthesis as well as structure - activity relationship studies are presented. 相似文献
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Raman SB Nguyen MH Zhang Z Cheng S Jia HY Weisner N Iczkowski K Clancy CJ 《Molecular microbiology》2006,60(3):697-709
Candida albicans causes diverse mucosal and systemic diseases. Although this versatility likely depends upon carefully co-ordinated gene expression, epigenetic regulation in C. albicans remains poorly characterized. Screening a genomic expression library, we identified C. albicans Set1p as an immunogenic protein with homology to a lysine histone methyltransferase of Saccharomyces cerevisiae. In this study, we demonstrated that total immunoglobulin, IgG and IgM titers against a unique Set1p N-terminal fragment were significantly higher among patients with disseminated candidiasis (DC) or oropharyngeal candidiasis than controls. Disruption of SET1 resulted in complete loss of methylation of histone 3 at lysine residue 4, hyperfilamentous growth under embedded conditions, less negative cell surface charges and diminished adherence to epithelial cells, effects that were reversed upon gene re-insertion at a disrupted locus. During murine DC, the null mutant was associated with prolonged survival and lower tissue burdens. Taken together, our findings suggest that SET1 regulates multiple processes important to the pathogenesis of candidiasis. The Set1p N-terminal fragment does not exhibit significant homology to eukaryotic or microbial proteins, and might represent a novel therapeutic, preventive or diagnostic target. 相似文献
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Wang M Ng KK Cherney MM Chan L Yannopoulos CG Bedard J Morin N Nguyen-Ba N Alaoui-Ismaili MH Bethell RC James MN 《The Journal of biological chemistry》2003,278(11):9489-9495
X-ray crystal structures of two non-nucleoside analogue inhibitors bound to hepatitis C virus NS5B RNA-dependent RNA polymerase have been determined to 2.0 and 2.9 A resolution. These noncompetitive inhibitors bind to the same site on the protein, approximately 35 A from the active site. The common features of binding include a large hydrophobic region and two hydrogen bonds between both oxygen atoms of a carboxylate group on the inhibitor and two main chain amide nitrogen atoms of Ser(476) and Tyr(477) on NS5B. The inhibitor-binding site lies at the base of the thumb domain, near its interface with the C-terminal extension of NS5B. The location of this inhibitor-binding site suggests that the binding of these inhibitors interferes with a conformational change essential for the activity of the polymerase. 相似文献
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Yannopoulos CG Xu P Ni F Chan L Pereira OZ Reddy TJ Das SK Poisson C Nguyen-Ba N Turcotte N Proulx M Halab L Wang W Bédard J Morin N Hamel M Nicolas O Bilimoria D L'Heureux L Bethell R Dionne G 《Bioorganic & medicinal chemistry letters》2004,14(21):5333-5337
HCV NS5B RNA-dependent RNA polymerase (NS5B) is essential for viral replication and is therefore considered a target for antiviral drug development. From our ongoing screening effort in the search for new anti-HCV agents, a novel inhibitor 1 with low microM activity against the HCV NS5B polymerase was identified. SAR analysis indicated the optimal substitution pattern required for activity, for example, carboxylic acid group at 2-position of thiophene ring. We describe the steps taken to identify and solve the bioactive conformation of derivative 6 through the use of the transferred NOE method (trNOE). 相似文献
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Tarek S. Mansour Colleen A. Evans M. Arshad Siddiqui Marie Charron Boulos Zacharie Nghe Nguyen-Ba 《Nucleosides, nucleotides & nucleic acids》2013,32(7-9):993-1001
Abstract The structure-activity relationship of sixteen 3-deaza, C-4 substituted pyrimidines and imidazo[1,2-c]pyrimidine bases of 1,3-oxathiolanes and 1,3-dioxolanes revealed good anti-HBV activity in 2.2.15 cells transfected with human hepatitis B virus of the imidazo[1,2-c]pyrimidine nucleosides 21, 25 and 29. Two procedures for the preparation of C-4 substituted analogues are reported based on nucleophilic displacement of a sulfonamide or imidazole by a variety of nitrogen nucleophiles. 相似文献
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Paul Nguyen-Ba Nathalie Turcotte Leonard Yuen Jean Bédard Miguel Quimpère Laval Chan 《Bioorganic & medicinal chemistry letters》1998,8(24):113-3566
We have recently described the discovery of new leads in the area of anti-HCMV research. Further structure - activity relationship studies have allowed us to identify potent and selective anti-HCMV nucleotide analogs. The synthesis as well as structure - activity relationship studies are described. 相似文献
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Sarah Boulineau Filipe Tostevin Daniel J. Kiviet Pieter Rein ten Wolde Philippe Nghe Sander J. Tans 《PloS one》2013,8(4)
Stochasticity in gene regulation has been characterized extensively, but how it affects cellular growth and fitness is less clear. We study the growth of E. coli cells as they shift from glucose to lactose metabolism, which is characterized by an obligatory growth arrest in bulk experiments that is termed the lag phase. Here, we follow the growth dynamics of individual cells at minute-resolution using a single-cell assay in a microfluidic device during this shift, while also monitoring lac expression. Mirroring the bulk results, the majority of cells displays a growth arrest upon glucose exhaustion, and resume when triggered by stochastic lac expression events. However, a significant fraction of cells maintains a high rate of elongation and displays no detectable growth lag during the shift. This ability to suppress the growth lag should provide important selective advantages when nutrients are scarce. Trajectories of individual cells display a highly non-linear relation between lac expression and growth, with only a fraction of fully induced levels being sufficient for achieving near maximal growth. A stochastic molecular model together with measured dependencies between nutrient concentration, lac expression level, and growth accurately reproduces the observed switching distributions. The results show that a growth arrest is not obligatory in the classic diauxic shift, and underscore that regulatory stochasticity ought to be considered in terms of its impact on growth and survival. 相似文献