title: Polyamine-oligonucleotide conjugates: a promising direction for nucleic acid tools and therapeutics.
abstract: Chemical modification and/or the conjugation of small functional molecules to oligonucleotides have significantly improved their biological and biophysical properties, addressing issues such as poor cell penetration, stability to nucleases and low affinity for their targets. Here, the authors review the literature reporting on the biophysical, biochemical and biological properties of one particular class of modification - polyamine-oligonucleotide conjugates. Naturally derived and synthetic polyamines have been grafted onto a variety of oligonucleotide formats, including antisense oligonucleotides and siRNAs. In many cases this has had beneficial effects on their properties such as target hybridization, nuclease resistance, cellular uptake and activity. Polyamine-oligonucleotide conjugation, therefore, represents a promising direction for the further development of oligonucleotide-based therapeutics and tools.
authors.affiliation: Department of Chemistry & Applied Biosciences, ETH Zurich, CH-8093 Zurich, Switzerland.
authors.forename: Mirjam
authors.initials: M
authors.lastname: Menzi
authors.affiliation: Department of Chemistry & Applied Biosciences, ETH Zurich, CH-8093 Zurich, Switzerland.
authors.forename: Helen L
authors.initials: HL
authors.lastname: Lightfoot
authors.affiliation: Department of Chemistry & Applied Biosciences, ETH Zurich, CH-8093 Zurich, Switzerland.
authors.forename: Jonathan
authors.initials: J
authors.lastname: Hall
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods; D006801:Humans; D009696:Nucleic Acids / Q000737:chemistry* / Q000494:pharmacology*; D009841:Oligonucleotides / Q000737:chemistry* / Q000494:pharmacology*; D016376:Oligonucleotides, Antisense / Q000737:chemistry / Q000494:pharmacology; D011073:Polyamines / Q000737:chemistry* / Q000494:pharmacology*; D034741:RNA, Small Interfering / Q000737:chemistry / Q000494:pharmacology
chemical_list: D009696:Nucleic Acids; D009841:Oligonucleotides; D016376:Oligonucleotides, Antisense; D011073:Polyamines; D034741:RNA, Small Interfering