phosphorothioate oligonucleotides


Summary: Modified oligonucleotides in which one of the oxygens of the phosphate group is replaced with a sulfur atom.

Top Publications

  1. Schmidt K, Prakash T, Donner A, Kinberger G, Gaus H, Low A, et al. Characterizing the effect of GalNAc and phosphorothioate backbone on binding of antisense oligonucleotides to the asialoglycoprotein receptor. Nucleic Acids Res. 2017;45:2294-2306 pubmed publisher
    ..Our results provide insights into how backbone charge and chemical composition assist in the binding and internalization of highly polar anionic single stranded oligonucleotides into cells and tissues. ..
  2. Maruyama H, Oikawa R, Hayakawa M, Takamori S, Kimura Y, Abe N, et al. Chemical ligation of oligonucleotides using an electrophilic phosphorothioester. Nucleic Acids Res. 2017;45:7042-7048 pubmed publisher
    ..0-8.0 at room temperature, and resulted in a ligation product with a phosphoramidate bond with a 39-85% yield. This method has potential uses in biotechnology and chemical biology. ..
  3. Kellner S, DeMott M, Cheng C, Russell B, Cao B, You D, et al. Oxidation of phosphorothioate DNA modifications leads to lethal genomic instability. Nat Chem Biol. 2017;13:888-894 pubmed publisher
    ..The genotoxicity of HOCl in PT-containing bacteria suggests reduced fitness in competition with HOCl-producing organisms and during infections in humans. ..
  4. Iwamoto N, Butler D, Svrzikapa N, Mohapatra S, Zlatev I, Sah D, et al. Control of phosphorothioate stereochemistry substantially increases the efficacy of antisense oligonucleotides. Nat Biotechnol. 2017;35:845-851 pubmed publisher
    ..Further, we elucidated a triplet stereochemical code in the stereopure ASOs, 3'-SpSpRp, that promotes target RNA cleavage by RNase H1 in vitro and provides a more durable response in mice than stereorandom ASOs. ..
  5. Bailey J, Shen W, Liang X, Crooke S. Nucleic acid binding proteins affect the subcellular distribution of phosphorothioate antisense oligonucleotides. Nucleic Acids Res. 2017;45:10649-10671 pubmed publisher
  6. Järver P, O Donovan L, Gait M. A chemical view of oligonucleotides for exon skipping and related drug applications. Nucleic Acid Ther. 2014;24:37-47 pubmed publisher
  7. Velu C, Chaubey A, Phelan J, Horman S, Wunderlich M, Guzman M, et al. Therapeutic antagonists of microRNAs deplete leukemia-initiating cell activity. J Clin Invest. 2014;124:222-36 pubmed publisher
    ..These data establish microRNA as functional effectors of endogenous HOXA9 and HOX-based leukemia oncoproteins, provide a concise in vivo platform to test RNA therapeutics, and suggest therapeutic value for microRNA antagonists in AML. ..
  8. Wu Z, Lee M, Carruthers T, Szabo M, Dennis M, Swarbrick J, et al. New Lanthanide Tag for the Generation of Pseudocontact Shifts in DNA by Site-Specific Ligation to a Phosphorothioate Group. Bioconjug Chem. 2017;28:1741-1748 pubmed publisher
  9. Jairath V, Khanna R, Feagan B. Alicaforsen for the treatment of inflammatory bowel disease. Expert Opin Investig Drugs. 2017;26:991-997 pubmed publisher
    ..No major safety signals have been observed in UC patients treated with alicaforsen enemas. The potential as a novel therapy for pouchitis has led to orphan designation for this indication by the FDA and European Medicines Agency. ..