Identification of a dibenzocyclooctadiene lignan as a HIV-1 non-nucleoside reverse transcriptase inhibitor
| Autor: | Victor G. Kramer, Wei-Lie Xiao, Hongtao Xu, Yudong Quan, Maureen Oliveira, Thibault Mesplède, Ying-Shan Han, Susan P. Colby-Germinario, Han-Dong Sun, Mark A. Wainberg |
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| Rok vydání: | 2015 |
| Předmět: |
Drug Evaluation
Preclinical Human immunodeficiency virus (HIV) Biology Pharmacology medicine.disease_cause Lignans Cell Line Nucleoside Reverse Transcriptase Inhibitor Cyclooctanes Structure-Activity Relationship Species Specificity medicine Humans Drug toxicity EC50 Dibenzocyclooctadiene lignan Dose-Response Relationship Drug Original Articles General Medicine HIV Reverse Transcriptase Enzyme assay In vitro Mechanism of action Biochemistry HIV-2 HIV-1 biology.protein Reverse Transcriptase Inhibitors medicine.symptom |
| Zdroj: | Antiviral Chemistry and Chemotherapy. 24:28-38 |
| ISSN: | 2040-2066 |
| Popis: | Background Due to resistance to all classes of anti-HIV drugs and drug toxicity, there is a need for the discovery and development of new anti-HIV drugs. Methods HIV-1 inhibitors were identified and biologically characterized for mechanism of action. Results We identified a dibenzocyclooctadiene lignan, termed HDS2 that possessed anti-HIV activity against a wide variety of viral strains with EC50 values in the 1–3 µM range. HDS2 was shown to act as an NNRTI by qPCR and in vitro enzyme assays. Conclusions This compound provides a new scaffold for further optimization of activity through structure-guided design. |
| Databáze: | OpenAIRE |
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