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Nanomedicine (Lond) ; 14(9): 1095-1107, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-31066644

RESUMO

Aim: Polyanionic carbosilane dendrimers have been shown to be safe and block human immunodeficiency virus type 1 (HIV-1) infection in a multifunctional manner. The aim of this study is to evaluate the appearance of HIV-1 resistance mutations after treatment with polyanionic carbosilane dendrimers. Materials & methods: A resistance mutation assay was performed on MT2 cells, viral quantity was measured by ELISA HIVp24gag and titration was carried out on TZM.bl. Next generation sequencing for HIV-1 Env was performed on G1-S4 or G2-S16 dendrimers supernatants. Results: Data showed the appearance of mutation resistance to G1-S4 treatment, inducing three significant mutations. G2-S16 did not generate any mutations and, furthermore, inhibited G1-S4-resistant viruses. Conclusion: G1-S4 treatment generates significant mutations in HIV-1NL4.3. G2-S16 does not generate resistance-associated mutation, suggesting that G2-S16 is safe as a HIV-entry inhibitor.


Assuntos
Fármacos Anti-HIV/farmacologia , Dendrímeros/farmacologia , HIV-1/efeitos dos fármacos , Silanos/farmacologia , Linhagem Celular , Dendrímeros/química , Farmacorresistência Viral , Proteína gp120 do Envelope de HIV/genética , HIV-1/fisiologia , Humanos , Mutação , Silanos/química , Falha de Tratamento , Internalização do Vírus/efeitos dos fármacos
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