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Peter D. Williams Donnette D. Staas Shankar Venkatraman H. Marie Loughran Rowena D. Ruzek Theresa M. Booth Terry A. Lyle John S. Wai Joseph P. Vacca Bradley P. Feuston Linda T. Ecto Jessica A. Flynn Daniel J. DiStefano Daria J. Hazuda Carolyn M. Bahnck Amy L. Himmelberger Geetha Dornadula Renee C. Hrin Kara A. Stillmock Marc V. Witmer Jay A. Grobler 《Bioorganic & medicinal chemistry letters》2010,20(22):6754-6757
Optimization studies using an HIV RNase H active site inhibitor containing a 1-hydroxy-1,8-naphthyridin-2(1H)-one core identified 4-position substituents that provided several potent and selective inhibitors. The best compound was potent and selective in biochemical assays (IC50 = 0.045 μM, HIV RT RNase H; 13 μM, HIV RT-polymerase; 24 μM, HIV integrase) and showed antiviral efficacy in a single-cycle viral replication assay in P4-2 cells (IC50 = 0.19 μM) with a modest window with respect to cytotoxicity (CC50 = 3.3 μM). 相似文献
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Low pH is required for avian sarcoma and leukosis virus Env-dependent viral penetration into the cytosol and not for viral uncoating
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A novel entry mechanism has been proposed for the avian sarcoma and leukosis virus (ASLV), whereby interaction with specific cell surface receptors activates or primes the viral envelope glycoprotein (Env), rendering it sensitive to subsequent low-pH-dependent fusion triggering in acidic intracellular organelles. However, ASLV fusion seems to proceed to a lipid mixing stage at neutral pH, leading to the suggestion that low pH might instead be required for a later stage of viral entry such as uncoating (L. J. Earp, S. E. Delos, R. C. Netter, P. Bates, and J. M. White. J. Virol. 77:3058-3066, 2003). To address this possibility, hybrid virus particles were generated with the core of human immunodeficiency virus type 1 (HIV-1), a known pH-independent virus, and with subgroups A or B ASLV Env proteins. Infection of cells by these pseudotyped virions was blocked by lysosomotropic agents, as judged by inhibition of HIV-1 DNA synthesis. Furthermore, by using HIV-1 cores that contain a Vpr-beta-lactamase fusion protein (Vpr-BlaM) to monitor viral penetration into the cytosol, we demonstrated that virions bearing ASLV Env, but not HIV-1 Env, enter the cytosol in a low-pH-dependent manner. This effect was independent of the presence of the cytoplasmic tail of ASLV Env. These studies provide strong support for the model, indicating that low pH is required for ASLV Env-dependent viral penetration into the cytosol and not for viral uncoating. 相似文献
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Sireesh Dornadula Suresh Thiruppathi Rajaguru Palanisamy Dhamodharan Umapathy Takayoshi Suzuki Ramkumar K. Mohanram 《Journal of cellular physiology》2019,234(3):1996-2012
Pterostilbene (PTS), a naturally occurring stilbene, confers protection against oxidative and cytokine stress induced pancreatic β-cell apoptosis in vitro and in vivo. To provide insights into the molecular mechanism, we performed a proteomic study on the pancreas of PTS-treated diabetic mice using electrospray ionization tandem–mass spectrometry (LC–MS/MS). A total of 1,260 proteins were detected in triplicate samples. Of which, 359 proteins were found to be differentially regulated in streptozotocin-induced diabetic mice pancreas with two fold difference ( P < 0.05, two or more peptides) and on PTS treatment 315 proteins were normalized to control levels. Gene ontology (GO) indicated that majority of the differentially regulated proteins are involved in cellular functions such as metabolism, cellular structure, oxidative stress, endoplasmic-reticulum-associated protein degradation (ERAD) pathway and several stress sensors. Protein–protein interaction network analysis of these differentially expressed proteins showed clustering of proteins involved in protein processing in endoplasmic reticulum (protein synthesis machinery and protein folding), oxidative phosphorylation/oxidative stress proteins, oligosaccharide metabolic process, and antioxidant activity. Our results highlighted that PTS administration rehabilitated the defective metabolic process and redox imbalance, and also suppressed the unfolded protein response and ERAD pathways. The effects on targeting ER machinery and suppressing oxidative stress suggest the great potential of PTS for diabetes management. 相似文献
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In a subset of subjects on highly active antiretroviral therapy,human immunodeficiency virus type 1 RNA in plasma decays from 50 to <5 copies per milliliter,with a half-life of 6 months
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Di Mascio M Dornadula G Zhang H Sullivan J Xu Y Kulkosky J Pomerantz RJ Perelson AS 《Journal of virology》2003,77(3):2271-2275
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Intracellular expression of single-chain variable fragments to inhibit early stages of the viral life cycle by targeting human immunodeficiency virus type 1 integrase. 总被引:3,自引:1,他引:2
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P Levy-Mintz L Duan H Zhang B Hu G Dornadula M Zhu J Kulkosky D Bizub-Bender A M Skalka R J Pomerantz 《Journal of virology》1996,70(12):8821-8832
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