The Enterovirus 3C Protease Inhibitor SG85 Efficiently Blocks Rhinovirus Replication and Is Not Cross-Resistant with Rupintrivir
| Autor: | Céline Lacroix, Shyla George, Pieter Leyssen, Johan Neyts, Rolf Hilgenfeld |
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| Rok vydání: | 2015 |
| Předmět: |
Phenylalanine
Drug resistance Biology Virus Replication medicine.disease_cause Antiviral Agents Viral Proteins Drug Resistance Viral medicine Protease Inhibitors Pharmacology (medical) Enterovirus Pharmacology chemistry.chemical_classification Valine Isoxazoles Virology Pyrrolidinones Reverse genetics Protease inhibitor (biology) In vitro Amino acid Infectious Diseases Viral replication chemistry Rhinovirus medicine.drug |
| Zdroj: | Antimicrobial Agents and Chemotherapy. 59:5814-5818 |
| ISSN: | 1098-6596 0066-4804 |
| DOI: | 10.1128/aac.00534-15 |
| Popis: | The novel enterovirus protease inhibitor (PI) SG85 effectively inhibits the in vitro replication of 14 rhinoviruses representative of species A and B (median 50% effective concentration, 0.04 μM). A low-level SG85-resistant variant was selected that carried amino acid substitutions S127G and T143A in the 3C protease. Both substitutions are required for low-level resistance to SG85, as demonstrated by reverse genetics. Interestingly, there is no cross-resistance to SG85 and rupintrivir (another PI); a structural explanation is provided for this observation. |
| Databáze: | OpenAIRE |
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