Development of Antisense Oligonucleotides with Bridged Nucleic Acids
نویسندگان
چکیده
منابع مشابه
Amido-bridged nucleic acids with small hydrophobic residues enhance hepatic tropism of antisense oligonucleotides in vivo.
High scalability of a novel bicyclic nucleoside building block, amido-bridged nucleic acid (AmNA), to diversify pharmacokinetic properties of therapeutic antisense oligonucleotides is described. N2'-functionalization of AmNA with a variety of hydrophobic groups is straightforward. Combinations of these modules display similar antisense knockdown effects and improve cellular uptake, relative to ...
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The design of antisense oligonucleotides containing locked nucleic acids (LNA) was optimized and compared to intensively studied DNA oligonucleotides, phosphorothioates and 2'-O-methyl gapmers. In contradiction to the literature, a stretch of seven or eight DNA monomers in the center of a chimeric DNA/LNA oligonucleotide is necessary for full activation of RNase H to cleave the target RNA. For ...
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Novel 2'-O,4'-C-ethylene nucleosides have been synthesized as building blocks for antisense and antigene oligonucleotides. 2'-O,4'-C-Ethylene-bridged nucleic acids (ENA) comprising 2'-O,4'-C-ethylene nucleosides have considerable affinity to complementary RNA and double-stranded DNA. Incorporation of 2'-O,4'-C-ethylene nucleosides into oligonucleotides dramatically increase their resistance aga...
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PNA is a nucleic acid analog with an achiral polyamide backbone consisting of N-(2-aminoethyl)glycine units (figure 1). The purine or pyrimidine bases are linked to the each unit via a methylene carbonyl linker (1-3) to target the complementary nucleic acid (4). PNA binds to complementary RNA or DNA in a parallel or antiparallel orientation following the Watson-Crick base-pairing rules (5-7). T...
متن کاملCyclohexenyl nucleic acids: conformationally flexible oligonucleotides
Cyclohexenyl nucleic acid (CeNA) is a nucleic acid mimic, where the (deoxy)ribose sugar has been replaced by cyclohexenyl moieties. In order to study the conformation of cyclohexenyl nucleosides by NMR, the HexRot program was developed to calculate conformations from scalar coupling constants of cyclohexenyl compounds, analogous to the methods applied for (deoxy)ribose nucleosides. The conforma...
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ژورنال
عنوان ژورنال: Drug Delivery System
سال: 2020
ISSN: 0913-5006,1881-2732
DOI: 10.2745/dds.35.82