Substituted naphthalenones as a new structural class of HIV-1 reverse transcriptase inhibitors
| Autor: | Thomas G. Gant, Bechtold Clifford M, A K Patick, Hui Li, M. Alam, M. Skoog, Pin-Fang Lin, John J. Trimble, Richard J. Colonno, Albert I. Meyers |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Nevirapine
Pyridines T-Lymphocytes Naphthalenes Biology Antiviral Agents Cell Line Benzodiazepines Virology medicine Humans Cytotoxic T cell Binding site Oxazoles Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug Imidazoles Nucleotidyltransferase Molecular biology HIV Reverse Transcriptase Reverse transcriptase Enzyme chemistry Enzyme inhibitor HIV-1 biology.protein Reverse Transcriptase Inhibitors Primer (molecular biology) medicine.drug |
| Zdroj: | Antiviral Research. 22:131-141 |
| ISSN: | 0166-3542 |
| DOI: | 10.1016/0166-3542(93)90091-v |
| Popis: | A novel substituted naphthalenone (TGG-II-23A) has been found that inhibits HIV-1 infection of CEM-SS cells at concentrations that are not cytotoxic. Time of addition experiments indicate that TGG-II-23A functions at a stage of the HIV-1 life cycle at or near reverse transcription. Cell free assays confirmed that TGG-II-23A inhibits HIV-1 reverse transcriptase. Similar to other non-nucleoside inhibitors, TGG-II-23A was specific for HIV-1 and failed to inhibit the replication of HIV-2. The binding site of TGG-II-23A appears to be in close proximity to that of the TIBO-like inhibitors, since a TIBO-resistant HIV-1 was also resistant to TGG-II-23A treatment. TGG-II-23A is a mixed non-competitive inhibitor that exhibits the same template:primer selectivity as other non-nucleoside inhibitors. TGG-II-23A therefore represents a new structural entry into the TIBO/Nevirapine class of inhibitors of HIV-1 reverse transcriptase. |
| Databáze: | OpenAIRE |
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