ArticleBioorganic & medicinal chemistry letters2014
Oligonucleotides conjugated with short chemically defined polyethylene glycol chains are efficient antisense agents.
Article in Bioorganic & medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
10 citing papers in PubMed, 28 citations in OpenAlex.
- Nanopore-Based Profiling of PEGylation in Nucleic Acid Therapeutics.Journal of the American Chemical Society · 2026Article
- Translational and clinical development of therapeutic siRNA and ASOs: current industry practices, perspectives, and recommendations.Nucleic acids research · 2025Article
- Trends and Commonalities of Approved and Late Clinical-Phase RNA Therapeutics.Pharmaceutics · 2025Review
- Striving for Uniformity: A Review on Advances and Challenges To Achieve Uniform Polyethylene Glycol.Organic process research & development · 2024Review
- PK-modifying anchors significantly alter clearance kinetics, tissue distribution, and efficacy of therapeutics siRNAs.Molecular therapy. Nucleic acids · 2022Article
- Use of Protamine in Nanopharmaceuticals-A Review.Nanomaterials (Basel, Switzerland) · 2021Review
- Improved Antitumor Activity of the Fluoropyrimidine Polymer CF10 in Preclinical Colorectal Cancer Models through Distinct Mechanistic and Pharmacologic Properties.Molecular cancer therapeutics · 2021Article
- Transport Oligonucleotides-A Novel System for Intracellular Delivery of Antisense Therapeutics.Molecules (Basel, Switzerland) · 2020Article
- Article
- PEGylation of therapeutic oligonucletides: From linear to highly branched PEG architectures.Nano research · 2018Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Ligand conjugation is an attractive approach to rationally modify the poor pharmacokinetic behavior and cellular uptake properties of antisense oligonucleotides. Polyethylene glycol (PEG) attachment is a method to increase solubility of oligonucleotides and prevent the rapid elimination, thus increasing tissue distribution. On the other hand, the attachment of long PEG chains negatively influences the pharmacodynamic effect by reducing the hybridization efficiency. We examined the use of short PEG ligands on the in vitro effect of antisense agents. Circular dichroism showed that the tethering of PEG12-chains to phosphodiester and phosphorothioate oligonucleotides had no influence on their secondary structure and did not reduce the affinity to the counter strand. In an in vitro tumor model, a luciferase reporter assay indicated unchanged gene silencing activity compared to unmodified compounds, and even slightly superior target down regulation was found after treatment with a phosphorothioate modified conjugate.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.