Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227)Scott D Seiwert
InterMune, Inc, 3280 Bayshore Blvd, Brisbane, CA 94005, USA
Antimicrob Agents Chemother 52:4432-41. 2008
..These preclinical characteristics compare favorably to those of other inhibitors of NS3/4A in clinical development and therefore support the clinical investigation of ITMN-191 for the treatment of chronic hepatitis C...
HCV NS5B polymerase inhibitors 1: Synthesis and in vitro activity of 2-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivativesGuangyi Wang
Discovery Research, InterMune, Inc, Brisbane, CA 94005, USA
Bioorg Med Chem Lett 19:4476-9. 2009
..2-(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives as potential anti-HCV drugs targeting NS5B polymerase have been investigated. Their synthesis, HCV NS5B polymerase inhibition and replicon activity are discussed...
HCV NS5B polymerase inhibitors 2: Synthesis and in vitro activity of (1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl) azolo[1,5-a]pyridine and azolo[1,5-a]pyrimidine derivativesGuangyi Wang
Discovery Research, InterMune, Inc, Brisbane, CA 94005, USA
Bioorg Med Chem Lett 19:4480-3. 2009
..1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl) azolo[1,5-a]pyridine and azolo[1,5-a]pyrimidine derivatives have been investigated as potential anti-HCV drugs. Their synthesis, HCV NS5B polymerase inhibition, and replicon activity are discussed...
Virologic escape during danoprevir (ITMN-191/RG7227) monotherapy is hepatitis C virus subtype dependent and associated with R155K substitutionSharlene R Lim
InterMune, Inc, Brisbane, California, USA
Antimicrob Agents Chemother 56:271-9. 2012
..These data indicate the ascendant importance of R155K for viral escape during danoprevir treatment and may have implications for the clinical use of this agent...
Inhibition and binding kinetics of the hepatitis C virus NS3 protease inhibitor ITMN-191 reveals tight binding and slow dissociative behaviorRavi Rajagopalan
InterMune Inc, 3280 Bayshore Boulevard, Brisbane, California 94005, USA
Biochemistry 48:2559-68. 2009
..Slow dissociation is not observed with closely related macrocyclic inhibitors of NS3, suggesting that members of this class may display distinct binding kinetics...
Optimization of the multiple enzymatic activities of the hepatitis C virus NS3 proteinShawn Misialek
InterMune, Brisbane, CA 94005, USA
Anal Biochem 394:138-40. 2009
..These conditions enable a particularly sensitive protease assay that uses picomolar concentrations of NS3...
HCV NS5B polymerase inhibitors 3: Synthesis and in vitro activity of 3-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivativesGuangyi Wang
Discovery Research, InterMune, Inc, Brisbane, CA 94005, USA
Bioorg Med Chem Lett 19:4484-7. 2009
..Their synthesis, HCV NS5B polymerase inhibition, and replicon activity are discussed...
Monitoring protein modification with allosteric ribozymesNarendra K Vaish
Sirna Therapeutics, Inc, 2950 Wilderness Place, Boulder, CO 80301, USA
Methods 32:428-36. 2004
..These significant differences from antibodies allow the pre-programmed development of conformation-state-specific protein detection reagents that can be used to investigate the activation-state of signal transduction components...
Danoprevir monotherapy decreases inflammatory markers in patients with chronic hepatitis C virus infectionCaralee J Schaefer
InterMune, Inc, Brisbane, California 94005, USA
Antimicrob Agents Chemother 55:3125-32. 2011
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Immunomodulatory activities of IFN-gamma1b in combination with type I IFN: implications for the use of IFN-gamma1b in the treatment of chronic HCV infectionsTony Wang
InterMune Inc, Brisbane, CA 94005, USA
J Interferon Cytokine Res 26:473-83. 2006
..These results suggest that addition of IFN-gamma1b to HCV treatment regimens may provide unique benefits...
Zeptomole detection of a viral nucleic acid using a target-activated ribozymeNarendra K Vaish
Sirna Therapeutics, Inc, Boulder, Colorado 80301, USA
RNA 9:1058-72. 2003
..6 x 10(6)-fold greater than that previously demonstrated by oligonucleotide-activated ribozymes, and one that is sufficient for molecular diagnostic applications...