Background: Antiretroviral therapy has transformed HIV-1 infection into a managed condition with near-normal life expectancy. However, a significant number of patients remain with limited therapeutic options due to HIV-1 resistance, side effects, or drug costs. Further, it is likely that current drugs will not retain efficacy, due to risks of side effects and transmitted resistance. Results: We describe compound 5660386 (3-ethyl-2-[3-(1, 3, 3-trimethyl-1, 3-dihydro-2H-indol-2-ylidene)-1-propen-1-yl]-1, 3-benzothiazol-3-ium) as a novel inhibitor of HIV-1 entry. Compound 5660386 inhibits HIV-1 entry in cell lines and primary cells, binds to HIV-1 envelope protein, and inhibits the interaction of GP120 to CD4. Further, compound 5660386 showed a unique and broad-range activity against primary HIV-1 isolates from different subtypes and geographical areas. Conclusion: Development of small-molecule entry inhibitors of HIV-1 such as 5660386 may lead to novel classes of anti-HIV-1 therapeutics. These inhibitors may be particularly effective against viruses resistant to current antiretroviral drugs and could have potential applications in both treatment and prevention.
CITATION STYLE
Heredia, A. L., Latinovic, O. S., Barbault, F., & De Leeuw, E. P. H. (2015). Anovel small-molecule inhibitor of hiv-1 entry. Drug Design, Development and Therapy, 9, 5469–5478. https://doi.org/10.2147/DDDT.S89338
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