Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
| Autor: | Lori J. Gabryelski, Peter J. Felock, Daria J. Hazuda, Carol Blau, Jay A. Grobler, Abigail Wolfe, Michael D. Miller, Marc V. Witmer, William A. Schleif, Amy S. Espeseth, Kara A. Stillmock |
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| Rok vydání: | 2000 |
| Předmět: |
Transcription
Genetic Anti-HIV Agents T-Lymphocytes Virus Integration Integrase inhibitor HIV Integrase Virus Replication Catalysis Raltegravir Potassium Acetoacetates medicine Tumor Cells Cultured Humans Pyrroles HIV Integrase Inhibitors HIV Long Terminal Repeat chemistry.chemical_classification Multidisciplinary biology Drug Resistance Microbial Raltegravir Virology Coculture Techniques Recombinant Proteins Integrase Enzyme Viral replication chemistry Biochemistry Enzyme inhibitor DNA Viral Mutation biology.protein HIV-1 DNA Circular medicine.drug |
| Zdroj: | Science (New York, N.Y.). 287(5453) |
| ISSN: | 0036-8075 |
| Popis: | Integrase is essential for human immunodeficiency virus–type 1 (HIV-1) replication; however, potent inhibition of the isolated enzyme in biochemical assays has not readily translated into antiviral activity in a manner consistent with inhibition of integration. In this report, we describe diketo acid inhibitors of HIV-1 integrase that manifest antiviral activity as a consequence of their effect on integration. The antiviral activity of these compounds is due exclusively to inhibition of one of the two catalytic functions of integrase, strand transfer. |
| Databáze: | OpenAIRE |
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