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Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus.
We herein report a novel double pro-drug approach applied to the anti-HCV agent 2'-beta-C-methyl guanosine. A phosphoramidate ProTide motif and a 6-O-methoxy base pro-drug moiety are combined toExpand
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INX-08189, a Phosphoramidate Prodrug of 6-O-Methyl-2′-C-Methyl Guanosine, Is a Potent Inhibitor of Hepatitis C Virus Replication with Excellent Pharmacokinetic and Pharmacodynamic Properties
ABSTRACT INX-08189 is an aryl-phosphoramidate of 6-O-methyl-2′-C-methyl guanosine. INX-08189 was highly potent in replicon assays, with a 50% effective concentration of 10 ± 6 nM against hepatitis CExpand
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Phosphoramidate ProTides of 2'-C-methylguanosine as highly potent inhibitors of hepatitis C virus. Study of their in vitro and in vivo properties.
Hepatitis C virus infection constitutes a serious health problem in need of more effective therapies. Nucleoside analogues with improved exposure, efficacy, and selectivity are recognized as likelyExpand
  • 45
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Highly Selective Artificial K(+) Channels: An Example of Selectivity-Induced Transmembrane Potential.
  • A. Gilles, M. Barboiu
  • Medicine, Chemistry
  • Journal of the American Chemical Society
  • 13 January 2016
Natural KcsA K(+) channels conduct at high rates with an extraordinary selectivity for K(+) cations, excluding the Na(+) or other cations. Biomimetic artificial channels have been designed in orderExpand
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An artificial primitive mimic of the Gramicidin-A channel.
Gramicidin A (gA) is the simplest known natural channel, and important progress in improving conduction activity has previously been obtained with modified natural gAs. However, simple artificialExpand
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Multilayer lectin-glyconanoparticles architectures for QCM enhanced detection of sugar-protein interaction.
Multivalent biorecognition of lectin layers by glyconanoparticle sugar-clusters has been used to generate multilayer nanoplatform architectures in a QCM sensing setup.
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Dual pro-drugs of 2'-C-methyl guanosine monophosphate as potent and selective inhibitors of hepatitis C virus.
We have previously reported the power of combining a 5'-phosphoramidate ProTide, phosphate pro-drug, motif with a 6-methoxy purine pro-drug entity to generate highly potent anti-HCV agents, leadingExpand
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Dynamic constitutional electrodes toward functional fullerene wires.
Constitutional mesoporous thin-layer electrodes have been used to generate confined fullerene wires allowing a capacitive diffusion of electrons.
  • 11
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Targeting the Human 80S Ribosome in Cancer: From Structure to Function and Drug Design for Innovative Adjuvant Therapeutic Strategies
The human 80S ribosome is the cellular nucleoprotein nanomachine in charge of protein synthesis that is profoundly affected during cancer transformation by oncogenic proteins and provides cancerousExpand
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  • Open Access