A novel small-molecule inhibitor of HIV-1 entry.
Drug Des Devel Ther
; 9: 5469-78, 2015.
Article
em En
| MEDLINE
| ID: mdl-26491257
ABSTRACT
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.Palavras-chave
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
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Infecções por HIV
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HIV-1
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Inibidores da Fusão de HIV
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Benzotiazóis
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Internalização do Vírus
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article