Artículo
Glucose conjugation of anti-HIV-1 oligonucleotides containing unmethylated CpG motifs reduces their immunostimulatory activity
Autor/es | Reyes Darias, J. A.
Sánchez Luque, Francisco J. Morales, Juan C. Pérez Rentero, Sonia Eritja Casadellà, Ramón Berzal Herranz, Alfredo |
Fecha de publicación | 2015 |
Fecha de depósito | 2018-08-13 |
Publicado en |
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Resumen | Antisense 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 ... Antisense 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. |
Agencias financiadoras | Consejo Superior de Investigaciones Científicas (CSIC) |
Cita | Reyes 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. |
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