Reyes Darias, J. A.Sánchez Luque, Francisco J.Morales, Juan C.Pérez Rentero, SoniaEritja Casadellà, RamónBerzal Herranz, Alfredo2018-08-132018-08-132015Reyes Darias, J.A., Sánchez Luque, F.J., Morales, J.C., Pérez Rentero, S., Eritja Casadellà, R. y Berzal Herranz, A. (2015). Glucose conjugation of anti-HIV-1 oligonucleotides containing unmethylated CpG motifs reduces their immunostimulatory activity. Chembiochem, 16 (5), 584-591.1439-4227 (impreso)1439-7633 (electrónico)https://hdl.handle.net/11441/78042Antisense oligodeoxynucleotides (ODNs) are short synthetic DNA polymers complementary to a target RNA sequence. They are commonly designed to halt a biological event, such as translation or splicing. ODNs are potentially useful therapeutic agents for the treatment of different human diseases. Carbohydrate-ODN conjugates have been reported to improve the cell-specific delivery of ODNs through receptor mediated endocytosis. We tested the anti-HIV activity and biochemical properties of the 5′-end glucose-conjugated GEM 91 ODN targeting the initiation codon of the gag gene of HIV-1 RNA in cell-based assays. The conjugation of a glucose residue significantly reduces the immunostimulatory effect without diminishing its potent anti-HIV-1 activity. No significant effects were observed in either ODN stability in serum, in vitro degradation of antisense DNA-RNA hybrids by RNase H, cell toxicity, cellular uptake and ability to interfere with genomic HIV-1 dimerisation.application/pdfengAttribution-NonCommercial-NoDerivatives 4.0 Internacionalhttp://creativecommons.org/licenses/by-nc-nd/4.0/Glucose DNA oligonucleotidesHIV-1 inhibitionImmune response reductionConjugated oligonucleotidesinfo:eu-repo/semantics/articleinfo:eu-repo/semantics/openAccesshttps://doi.org/10.1002/cbic.201402574