AI Article Synopsis
- Researchers have discovered a new class of quinolizidines, such as aloperine, that can inhibit HIV infection by preventing the virus from entering human cells.
- They optimized the structure of aloperine and created a derivative that exhibits about 15 times stronger anti-HIV-1 activity.
- The study suggests that this compound does not stop HIV from binding to cell receptors but rather prevents the virus from fusing with the cell membrane, possibly by binding to the HIV-1 gp120 protein.
Article Abstract
As a step toward developing novel anti-HIV agents, we have identified a class of quinolizidines, including aloperine, that inhibit HIV at 1-5 μM by blocking viral entry. In this study, we have optimized the structure of aloperine and derived compounds with markedly improved activity. Our structural optimization has yielded an aloperine derivative with approximately a 15-fold increase in anti-HIV-1 activity. Our mechanism of action study reveals that compound does not inhibit binding of HIV-1 to receptors but arrests the virus from fusion with the membrane. Binding of the compound to HIV-1gp120 might be responsible for its anti-HIV-1 entry activity.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5683702 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.7b00376 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!