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Interaktion von c-Src mit der viralen Polymerase NS5B des Hepatitis C Virus und Generierung NS5B-spezifischer humaner Antikörperfragmente

, 2010
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Isothiazoles as active-site inhibitors of HCV NS5B polymerase

Bioorganic and Medicinal Chemistry Letters, 2007
Isothiazole analogs were discovered as a novel class of active-site inhibitors of HCV NS5B polymerase. The best compound has an IC(50) of 200 nM and EC(50) of 100 nM, which is a significant improvement over the starting inhibitor (1). The X-ray complex structure of 1 with HCV NS5B was obtained at a resolution of 2.2A, revealing that the inhibitor is ...
Shunqi Yan
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HCV NS5B Polymerase Inhibitors

Clinics in Liver Disease, 2009
Chronic hepatitis C virus (HCV) infection affects approximately 4 million persons and is the major indication for liver transplantation in the United States. The current standard for treatment of HCV is pegylated interferon in combination with ribavirin.
James R, Burton, Gregory T, Everson
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Quinolones as HCV NS5B polymerase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2011
Hepatitis C virus (HCV) infection is treated with a combination of peginterferon alfa-2a/b and ribavirin. To address the limitations of this therapy, numerous small molecule agents are in development, which act by directly affecting key steps in the viral life-cycle.
Dange V, Kumar, Roopa, Rai, Ken A, Brameld, John R, Somoza, Ravi, Rajagopalan, James W, Janc, Yu M, Xia, Tony L, Ton, Michael B, Shaghafi, Huiyong, Hu, Isabelle, Lehoux, Nhat, To, Wendy B, Young, Michael J, Green   +13 more
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1,5-Benzodiazepine inhibitors of HCV NS5B polymerase

Bioorganic & Medicinal Chemistry Letters, 2009
Optimization through parallel synthesis of a novel series of hepatitis C virus (HCV) NS5B polymerase inhibitors led to the identification of (R)-11-(4-benzyloxy-2-fluorophenyl)-6-hydroxy-3,3-dimethyl-10-(6-methylpyridine-2-carbonyl)-2,3,4,5,10,11-hexahydro-dibenzo[b,e][1,4]diazepin-1-one 11zc and (R)-11-(4-benzyloxy-2-fluorophenyl)-6-hydroxy-3,3 ...
Mcgowan, David, Nyanguile, Origene, Cummings, Maxwell D, Vendeville, Sandrine, Vandyck, Koen, Van Den Broeck, Walter, Boutton, Carlo W., De Bondt, Hendrik, Quirynen, Ludo, Amssoms, Katie, Bonfati, Jean-Francois, Last, Stefaan, Rombauts, Klara, Tahri, Abdellah, Hu, Lili, Delouvroy, Frederic, Vermeiren, K., Vandercruyssen, Genevieve, Van Der Helm, Liesbet, Cleiren, Erna, Mostmans, Wendy, Lory, Pedro, Pille, Geert, Van Emelen, Kristof, Fanning, Gregory, Pauwels, Frederik, Lin, Tse-I, Simmen, Kenneth, Raboisson, Pierre   +28 more
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New NS5B polymerase inhibitors for hepatitis C

Expert Opinion on Investigational Drugs, 2010
The current treatment of chronic hepatitis C based on the combination of pegylated interferon and ribavirin is effective in only 50% of patients. Specific targeted antiviral therapies represent a promising approach to eradicate the infection.This review focuses on progress towards the development of the hepatitis C virus (HCV) polymerase inhibitors ...
Florence, Legrand-Abravanel, Florence, Nicot, Jacques, Izopet   +2 more
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Hepatitis C therapy with HCV NS5B polymerase inhibitors

Expert Opinion on Pharmacotherapy, 2013
Several HCV polymerase inhibitors are in advanced stages of clinical development. They are nucleos(t)ide and non-nucleoside analogs. Nucleos(t)ides inhibit viral replication acting as chain terminators whereas non-nucleosides block allosterically the HCV polymerase.
Soriano, Vincent, Vispo, Eugenia, de Mendoza, Carmen, Labarga, Pablo, Fernandez-Montero, Jose Vicente, Poveda, Eva, Treviño, Ana, Barreiro, Pablo   +7 more
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Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase

Bioorganic & Medicinal Chemistry Letters, 2006
A novel series of selective HCV NS5B RNA dependent RNA polymerase inhibitors has been disclosed. These compounds contain an appropriately substituted tetrahydrobenzothiophene scaffold. This communication will detail the SAR and activities of this series.
M G, Laporte, T A, Lessen, L, Leister, D, Cebzanov, E, Amparo, C, Faust, D, Ortlip, T R, Bailey, T J, Nitz, S K, Chunduru, D C, Young, C J, Burns   +11 more
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Current Perspective of HCV NS5B Inhibitors: A Review

Current Medicinal Chemistry, 2011
Hepatitis C virus (HCV) infection has emerged as one of the most significant disease to affect humans. Despite its large medical and economical impact, there are no vaccines or efficient therapies without major side effects. The HCV non-structural protein 5B (NS5B) is the RNA-dependent RNA polymerase responsible for the complete copy of the RNA viral ...
V M, Patil, S P, Gupta, S, Samanta, N, Masand   +3 more
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