165381-00-0Relevant academic research and scientific papers
Oligonucleotide charge reversal: 2′-O-lysylaminohexyl modified oligonucleotides
Winkler, Johannes,Noe, Christian R.
, p. 939 - 942 (2007)
A novel cationic building nucleoside building block designed for antisense and siRNA oligonucleotides is presented. Protected L-lysine was coupled to 2′-O-aminohexyluridine and the resulting nucleoside was phosphitylated for automated oligonucleotide synt
LIPIDIC NUCLEIC ACIDS
Manoharan, Muthiah,Tivel, Kathleen L.,Cook, P. Dan
, p. 3651 - 3654 (1995)
Lipophilic nucleosides were synthesized from uridine via either a 2'-O-hexylamino tether or the corresponding 3'-linker.These synthons allowed site-specific incorporation of the lipophilic moieties into antisence oligonucleotides.A spectrum of lipophilicity was observed in the oligonucleotides, depending on the pendent group.
Structural modifications of antisense oligonucleotides
Urban, Ernst,Noe, Christian R.
, p. 243 - 258 (2007/10/03)
Antisense oligonucleotides are efficient tools for the inhibition of gene expression in a sequence specific way. Natural oligonucleotides are decomposed rapidly in biological systems, which strongly restrict their application. In contrast, artificial oligonucleotides are designed to be more stable against degradation than the target mRNA, which results in a catalytic effect of the drug. Modification of the phosphate linkage has been the first successful strategy for antisense drug developments and Fomivirsene the first antisense drug in therapy. The launch of Fomivirsene has resulted in a revolutionary spin off to antisense research leading to a second generation of antisense oligonucleotides, which are stable against oligonucleotide cleaving enzymes. Among these, oligonucleotides bearing an alkoxy substituent in position 2′ were the most successful ones. The third generation of antisense oligonucleotides contains structure elements, which enhance the antisense action. Zwitterionic oligonucleotides show remarkable results, first, because the stability against ribozymes is largely increased, and secondly, because the electrostatic repulsion between the anionic sense and the zwitterionic antisense cords is minimized. Promising new target molecules in antisense reseach are oligonucleotide chimaeres, which enhance the antisense action (chimaeres with intercalators, chelators or polyamines) or enable an application as sequence specific detectors (chimaeres with biotin, fluorescein or radioligands).
Base-Sequence Dependence of Emission Lifetimes for DNA Oligomers and Duplexes Covalently Labeled with Pyrene: Relative Electron-Transfer Quenching Efficiencies of A, G, C, and T Nucleosides toward Pyrene
Manoharan, Muthiah,Tivel, Kathleen L.,Zhao, Min,Nafisi, Kambiz,Netzel, Thomas L.
, p. 17461 - 17472 (2007/10/02)
This paper reports both continuous and time-resolved spectroscopic studies of the emission properties of photoexcited pyrene labels covalently attached to uridine nucleosides and oligonucleotides.For all nucleic acid systems, uridine is substituted with p
