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Broad Antiretroviral Activity and Resistance Profile of the Novel Human Immunodeficiency Virus Integrase Inhibitor Elvitegravir (JTK-303/GS-9137)
The antiviral activity and resistance profile in vitro of a novel IN inhibitor, elvitegravir (EVG) (also known as JTK-303/GS-9137), currently being developed for the treatment of HIV-1 infection are described, suggesting that IN inhibitors bind to a conformationally conserved region of various retroviral IN enzymes and are an ideal drug for a range of Retroviral infections. Expand
Novel HIV-1 integrase inhibitors derived from quinolone antibiotics.
The modification of a quinolone antibiotic is described to produce the novel integrase inhibitor JTK-303 (GS 9137) that blocks strand transfer by the viral enzyme. Expand
Activity of a Sulfated Polysaccharide Extracted from the Red Seaweed Aghardhiella Tenera against Human Immunodeficiency Virus and Other Enveloped Viruses
GS represents a natural polysaccharide with broad-spectrum activity against a number of important viral pathogens and proved active not only against HIV-1 and HIV-2 but also against other enveloped viruses, i.e. herpes-, toga-, arena-, myxo- and rhabdoviruses. Expand
The essential role of C-terminal residues in regulating the activity of hepatitis C virus RNA-dependent RNA polymerase.
Structural comparison of the NS5B proteins indicates that the activation was caused by elimination of a unique hydrophobic interaction between the three C-terminal residues and a shallowly concave pocket consisting of thumb and palm domains. Expand
Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: structure-activity relationship studies and identification of a potent and
Among the new compounds, compound 10n (JTK-109) exhibited favorable pharmacokinetic profiles, high selectivity for NS5B, and good safety profiles, suggesting the potential for a clinical candidate in the treatment of hepatitis C. Expand
Effects of Mutation in Hepatitis C Virus Nonstructural Protein 5A on Interferon Resistance Mediated by Inhibition of PKR Kinase Activity in Mammalian Cells
Observations confirmed the previous report that the inhibitory effect of NS5A on IFN activity is mediated at least in part by the repression of PKR, and showed that IFN sensitivity was determined not only by the ISDR but that the involvement of the C‐terminal region ofNS5A‐1b is important for the suppression ofPKR activity. Expand
Quinolone carboxylic acids as a novel monoketo acid class of human immunodeficiency virus type 1 integrase inhibitors.
The synthesis and the detailed structure-activity relationship of the quinolone carboxylic acids are shown as a novel monoketo acid class of integrase inhibitors and Elvitegravir 49 was chosen as a candidate for further studies and is currently in phase 3 clinical trials. Expand
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors.
A new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold and displaying a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin. Expand
MDM2 is a novel E3 ligase for HIV-1 Vif
The data suggest that MDM2 is a regulator of HIV-1 replication and might be a novel therapeutic target for anti-HIV-1 drug, and the mechanisms by whichMDM2 only targets Vif, but not A3G that binds to Vif. Expand
Antiviral activity of a sulphated polysaccharide from the red seaweed Nothogenia fastigiata.
The antiviral activity of polysaccharide fractions obtained from water extracts of the red seaweed Nothogenia fastigiata was investigated. Fraction F6, corresponding to a sulphated xylomannan, wasExpand