Results 141 to 150 of about 9,676 (179)

Enantioselective Synthesis of an HCV NS5a Antagonist

Organic Letters, 2014
A concise, enantioselective synthesis of the HCV NS5a inhibitor MK-8742 (1) is reported. The features of the synthesis include a highly enantioselective transfer hydrogenation of an NH imine and a dynamic diastereoselective transformation. The synthesis of this complex target requires simple starting materials and nine linear steps for completion.
Ian K, Mangion, Cheng-yi, Chen, Hongmei, Li, Peter, Maligres, Yonggang, Chen, Melodie, Christensen, Ryan, Cohen, Ingyu, Jeon, Artis, Klapars, Shane, Krska, Hoa, Nguyen, Robert A, Reamer, Benjamin D, Sherry, Ilia, Zavialov   +13 more
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In Silico Approaches to the Design of NS5A Inhibitors

Current Topics in Medicinal Chemistry, 2016
In recent years, nonstructural protein 5A (NS5A) has rapidly emerged as a promising therapeutic target for Hepatitis C (HCV) virus therapy. It is involved in both viral RNA replication and virus assembly and NS5A plays a critical role in the regulation of HCV life cycle. NS5A replication complex inhibitors (NS5A RCIs) have demonstrated strong antiviral
Yan A, Ivanenkov, Mark S, Veselov, Vladimir A, Aladinskiy, Artem G, Shakhbazyan, Sofya M, Yartseva, Alexander G, Majouga, Anastasia V, Aladinskaya, Anton S, Vantskul, Sergey V, Leonov, Alexandre V, Ivachtchenko, Victor E, Koteliansky   +10 more
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HCV NS5A replication complex inhibitors

Current Opinion in Pharmacology, 2016
The development of anti-HCV drugs is one of the most successful stories of antiviral therapy. In fact, for the first time in human history we have the potential to eradicate a chronic viral infection using only orally administered direct antiviral agents (DAAs).
Min, Gao, Donald R, O'Boyle, Susan, Roberts   +2 more
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Discovery of fluorobenzimidazole HCV NS5A inhibitors

Bioorganic & Medicinal Chemistry Letters, 2016
Research toward a next-generation HCV NS5A inhibitor has identified fluorobenzimidazole analogs that demonstrate potent, broad-genotype in vitro activity against HCV genotypes 1-6 replicons as well as HCV NS5A variants that are orders of magnitude less susceptible to inhibition by first-generation NS5A inhibitors in comparison to wild-type replicons ...
John T, Randolph, Charles A, Flentge, Pamela, Donner, Todd W, Rockway, Sachin V, Patel, Lissa, Nelson, Douglas K, Hutchinson, Rubina, Mondal, Neeta, Mistry, Thomas, Reisch, Tatyana, Dekhtyar, Preethi, Krishnan, Tami, Pilot-Matias, Deanne F, Stolarik, David W A, Beno, Rolf, Wagner, Clarence, Maring, Warren M, Kati   +17 more
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[Expression of HCV NS5A gene in HepG2 cell and the effect of the NS5A expression on PI3K in vitro].

Xi bao yu fen zi mian yi xue za zhi = Chinese journal of cellular and molecular immunology, 2009
To reveal the influence of HCV-NS5A on PI3K, we probe into the relationship between NS5A and PI3K in vitro.Full length NS5A gene of HCV was amplified by PCR, using the plasmid containing HCV full-length open reading frame (ORF) as template, and cloned into the eukaryotic expressing plasmid pcDNA3.0(-) by DNA recombination technique.
Xue-Fang, Hu, Xiao-Zhao, Deng, Zhen-Yu, Diao, Yun, Zhang, Zong-An, Zhou, Yu, Liu   +5 more
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HCV NS5A Inhibitors in Development

Clinics in Liver Disease, 2013
NS5A protein plays a key role in hepatitis C virus (HCV) replication. Daclatasvir (DCV, BMS-790052) is a first-in-class inhibitor of the HCV NS5A replication complex with potent antiviral activity but a low barrier to resistance. DCV as triple therapy in combination with pegylated interferon and ribavirin resulted in a high rate of early virologic ...
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The NS5A Replication Complex Inhibitors: Difference Makers?

Clinics in Liver Disease, 2011
The development and approval of direct-acting antiviral agents looks set to transform the treatment of chronic hepatitis C infection. Among the agents in development are novel compounds that inhibit the function of the NS5A protein: a pleiotropic protein with a complex and essential role in viral replication.
Robert G, Gish, Nicholas A, Meanwell
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Ser235 phosphorylation of hepatitis C virus NS5A is required for NS5A dimerization and drug resistance

Life Sciences
Hepatitis C virus (HCV) infection is recognized as a major causative agent of chronic hepatitis, cirrhosis, and hepatocellular carcinoma. HCV non-structural protein 5A (NS5A) is a dimeric phosphoprotein with a hyperphosphorylated form to act as a switch that regulates HCV replication and assembly.
Wei-Ping, Lee, Keng-Chang, Tsai, Shi-Xian, Liao, Yi-Hsiang, Huang, Ming-Chih, Hou, Keng-Hsin, Lan   +5 more
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The hepatitis C virus NS5A inhibitor (BMS-790052) alters the subcellular localization of the NS5A non-structural viral protein

Virology, 2011
The hepatitis C virus (HCV) non-structural (NS) 5A protein plays an essential role in the replication of the viral RNA by the membrane-associated replication complex (RC). Recently, a putative NS5A inhibitor, BMS-790052, exhibited the highest potency of any known anti-HCV compound in inhibiting HCV replication in vitro and showed a promising clinical ...
Choongho Lee, Vincent Leveque, Ella H Sklan   +2 more
exaly   +3 more sources

NS5A Phosphorylation and Hyperphosphorylation

2009
NS5A phosphorylation can be studied in two ways: in living cells and in vitro. The former has several advantages: NS5A phosphorylation takes place in a cellular background and therefore might mimic more closely the real in vivo situation. Viral proteins and cellular kinases are in the correct cellular compartments, and dynamic processes like viral ...
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