ArticlePloS one2014
Delivery of antisense peptide nucleic acids to cells by conjugation with small arginine-rich cell-penetrating peptide (R/W)9.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 32 citations in OpenAlex.
- Design, Synthesis and Biophysical Characterisation of CPP-PNA Conjugates for Targeting Oncogenic microRNA-221.Journal of peptide science : an official publication of the European Peptide Society · 2026Article
- Sequence specificity of peptide nucleic acids containing terminal cationic amino acids.Bioorganic & medicinal chemistry · 2026Article
- The Internal Nanostructure of Lipid Nanoparticles Influences Their Diverse Cellular Uptake Pathways.Small (Weinheim an der Bergstrasse, Germany) · 2025Article
- AntimiR uptake by human proximal tubule epithelial cells is predominantly by macropinocytosis.Scientific reports · 2025Article
- Peptide-conjugated antimiRs improve myotonic dystrophy type 1 phenotypes by promoting endogenous MBNL1 expression.Molecular therapy. Nucleic acids · 2023Article
- Peptide nucleic acid conjugates and their antimicrobial applications-a mini-review.European biophysics journal : EBJ · 2023Review
- Article
- Transcript-Targeted Therapy Based on RNA Interference and Antisense Oligonucleotides: Current Applications and Novel Molecular Targets.International journal of molecular sciences · 2022Review
- Head on Comparison of Self- and Nano-assemblies of Gamma Peptide Nucleic Acid Amphiphiles.Advanced functional materials · 2022Article
- Chemistry of Peptide-Oligonucleotide Conjugates: A Review.Molecules (Basel, Switzerland) · 2021Review
- Antibacterial Peptide Nucleic Acids-Facts and Perspectives.Molecules (Basel, Switzerland) · 2020Review
- Spontaneous driving forces give rise to protein-RNA condensates with coexisting phases and complex material properties.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Role of Cell-Penetrating Peptides in Intracellular Delivery of Peptide Nucleic Acids Targeting Hepadnaviral Replication.Molecular therapy. Nucleic acids · 2017Article
- The novel functional nucleic acid iRed effectively regulates target genes following cytoplasmic delivery by faint electric treatment.Science and technology of advanced materials · 2016Article
- Delivery of cell-penetrating peptide-peptide nucleic acid conjugates by assembly on an oligonucleotide scaffold.Scientific reports · 2015Article
- Peptides and Peptidomimetics for Antimicrobial Drug Design.Pharmaceuticals (Basel, Switzerland) · 2015Review
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Authors and funding
10 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Peptide nucleic acids (PNAs) are very attractive antisense and antigene agents, but these molecules are not passively taken into cells. Here, using a functional cell assay and fluorescent-based methods, we investigated cell uptake and antisense activity of a tridecamer PNA that targets the HIV-1 polypurine tract sequence delivered using the arginine-rich (R/W)9 peptide (RRWWRRWRR). At micromolar concentrations, without use of any transfection agents, almost 80% inhibition of the target gene expression was obtained with the conjugate in the presence of the endosomolytic agent chloroquine. We show that chloroquine not only induced escape from endosomes but also enhanced the cellular uptake of the conjugate. Mechanistic studies revealed that (R/W)9-PNA conjugates were internalized via pinocytosis. Replacement of arginines with lysines reduced the uptake of the conjugate by six-fold, resulting in the abolition of intracellular target inhibition. Our results show that the arginines play a crucial role in the conjugate uptake and antisense activity. To determine whether specificity of the interactions of arginines with cell surface proteoglycans result in the internalization, we used flow cytometry to examine uptake of arginine- and lysine-rich conjugates in wild-type CHO-K1 and proteoglycan-deficient A745 cells. The uptake of both conjugates was decreased by four fold in CHO-745 cells; therefore proteoglycans promote internalization of cationic peptides, irrespective of the chemical nature of their positive charges. Our results show that arginine-rich cell-penetrating peptides, especially (R/W)9, are a promising tool for PNA internalization.
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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.