Fusion and Entry inhibitors
New Small Molecule Entry Inhibitors Targeting Hemagglutinin-Mediated Influenza A Virus Fusion
... these inhibitors appear to bind directly to HA and block the HA conforma- tional ...These inhibitors include BMY 27709 (36), 180299 (a podocarpic acid derivative) (61), tert-butyl hydroquinone (TBHQ) (60), ...
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HIV Resistance to Entry Inhibitors
... HIV entry The need for new classes of antiretroviral drugs has become apparent from the increasing concern on the long term toxicity 1 and the spreading of HIV-1 variants that are resistant to current treatment ...
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Lysosomotropic agents as HCV entry inhibitors
... toxicological effects of Chloroquine and NH 4 Cl were tested in liver cells through MTT cell proliferation assay. For antiviral screening of Chloroquine and NH 4 Cl, liver cells were infected with HCVpp of 3a and 1a ...
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Identification of Clotrimazole Derivatives as Specific Inhibitors of Arenavirus Fusion
... viral entry of highly pathogenic arenaviruses allows blocking the pathogen before it can take control of the host cell and blunt innate and adaptive antiviral ...viral entry and show distinct specificities ...
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Molecular Determinants of Antiviral Potency of Paramyxovirus Entry Inhibitors
... The helical packing rearrangements triggered by receptor binding are likely to underlie the mechanism of the F structural transitions required for activation of HeV/NiV membrane fu- sion. Our results show that the ...
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Viral Entry Inhibitors Targeted to the Membrane Site of Action
... of fusion activation, thus overcoming this ...peptide fusion antivirals that inhibit im- portant pediatric respiratory pathogens, as well as emerging ...viral entry are likely to be safe antivirals ...
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Assessment of HIV-1 entry inhibitors by MLV/HIV-1 pseudotyped vectors
... acids. HIV-1 Env facilitates vector attachment to target cells and membrane fusion, which is initiated by the inter- action of HIV-1 Env with the CD4 receptor molecule on the surface of the target cell. CD4 ...
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Entry Inhibitors: A Perspective for Prevention of Hepatitis C Virus Infection in Organ Transplantation
... of inhibitors interfering with HCV entry are in preclinical and clinical ...25 Entry inhibitors offer a number of attractive ...viral entry may also allow cure of chronic HCV infection, ...
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Resistance to N peptide fusion inhibitors correlates with thermodynamic stability of the gp41 six helix bundle but not HIV entry kinetics
... In one case, the peptide-sensitive, pre-hairpin intermediate might indeed have a longer lifetime, but resistance can be explained by an equilibrium between the peptide-sensitive, pre-hairpin intermediate and a later, ...
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Identification of Novel Fusion Inhibitors of Influenza A Virus by Chemical Genetics
... novel fusion inhibitors of influenza A ...novel fusion inhibitors of influenza A virus that act by interfering with the structural change of HA at acidic pH, a process necessary for successful ...
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Fatal Measles Virus Infection Prevented by Brain-Penetrant Fusion Inhibitors
... MV entry and spreading and MV-induced cell ...MV fusion protein, conjugated to cholesterol, efficiently protect SLAM transgenic mice from fatal MV ...infection. Fusion inhibitors hold promise ...
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Application of Click Chemistry in the Development of Peptide Based HIV Fusion Inhibitors
... envelope fusion with the CD4 cell membrane prevents the entry of HIV into the CD4 cells providing a novel approach to the treatment of HIV ...the fusion of the virus with the co-receptor substrate ...
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Peptide Inhibitors of Flavivirus Entry Derived from the E Protein Stem
... dengue entry, but mutation of their C-terminal residues to the DV2 consensus sequence or to sequences with enhanced hydrophobicity confers inhibitory ...membrane fusion. This mechanism sug- gests strategies ...
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pH-Induced Activation of Arenavirus Membrane Fusion Is Antagonized by Small-Molecule Inhibitors
... viral entry through pH-induced membrane fusion in the ...membrane fusion by targeting the interaction of the G2 fusion subunit with the stable signal peptide ...
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pH-Induced Activation of Arenavirus Membrane Fusion is antagonized by Small-Molecule Inhibitors
... viral entry through pH-induced membrane fusion in the ...membrane fusion by targeting the interaction of the G2 fusion subunit with the stable signal peptide ...
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HveA (Herpesvirus Entry Mediator A), a Coreceptor for Herpes Simplex Virus Entry, also Participates in Virus-Induced Cell Fusion
... (HSV-1) entry, herpesvirus entry mediator (previously designated HVEM but renamed HveA), also mediates HSV-1-induced cell-cell ...effective inhibitors of KOS-804-induced fusion, consistent ...
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Abelson Kinase Inhibitors Are Potent Inhibitors of Severe Acute Respiratory Syndrome Coronavirus and Middle East Respiratory Syndrome Coronavirus Fusion
... kinase inhibitors have previously been shown to inhibit replication of Ebola virus (14, 15), coxsackievirus (16), and vaccinia virus (17), but at different points of the virus life ...virion fusion with the ...
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Low-pH Triggering of Human Metapneumovirus Fusion: Essential Residues and Importance in Entry
... acidification inhibitors in a more physiologically relevant cell ...cation inhibitors on HMPV infection in A549 cells, a human alveolar type II-like epithelial cell line, which others have char- acterized ...
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Genetic Pathway of HIV-1 Resistance to Novel Fusion Inhibitors Targeting the Gp41 Pocket
... tion, N163D, might significantly improve the functionality of viral Env glycoprotein to mediate the fusion. We think that the binding affinity, the structural changes, and the viral fusion kinetics are ...
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Novel Inhibitors of Influenza Virus Fusion: Structure-Activity Relationship and Interaction with the Viral Hemagglutinin
... DISCUSSION Fusion between the viral and endosomal membranes is an essential event during influenza virus entry into the host cell. FIG. 5. pH dependence of hemolysis for wild-type and 4c-resistant mutants. ...
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