ArticleJournal of medicinal chemistry2012
A peptide nucleic acid-aminosugar conjugate targeting transactivation response element of HIV-1 RNA genome shows a high bioavailability in human cells and strongly inhibits tat-mediated transactivation of HIV-1 transcription.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 36 citations in OpenAlex.
- Aminoglycoside-Peptide Nucleic Acid (PNA) Conjugates against Gram-Negative Bacteria.Bioconjugate chemistry · 2025Article
- Peptide nucleic acid conjugates and their antimicrobial applications-a mini-review.European biophysics journal : EBJ · 2023Review
- Chemical approaches to discover the full potential of peptide nucleic acids in biomedical applications.Beilstein journal of organic chemistry · 2021Review
- Amphiphilic Aminoglycosides as Medicinal Agents.International journal of molecular sciences · 2020Review
- RNA Secondary Structure-Based Design of Antisense Peptide Nucleic Acids for Modulating Disease-Associated Aberrant Tau Pre-mRNA Alternative Splicing.Molecules (Basel, Switzerland) · 2019Article
- Incorporating uracil and 5-halouracils into short peptide nucleic acids for enhanced recognition of A-U pairs in dsRNAs.Nucleic acids research · 2018Article
- Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids.Journal of visualized experiments : JoVE · 2017Article
- Incorporating a guanidine-modified cytosine base into triplex-forming PNAs for the recognition of a C-G pyrimidine-purine inversion site of an RNA duplex.Nucleic acids research · 2016Article
- Cellular uptake and intracellular trafficking of oligonucleotides: implications for oligonucleotide pharmacology.Nucleic acid therapeutics · 2014Review
- A simple strategy for glycosyltransferase-catalyzed aminosugar nucleotide synthesis.Chembiochem : a European journal of chemical biology · 2014Article
- Affinity capture and identification of host cell factors associated with hepatitis C virus (+) strand subgenomic RNA.Molecular & cellular proteomics : MCP · 2013Article
- Glycopolymer probes of signal transduction.Chemical Society reviews · 2013Review
Corrections and comments
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Authors and funding
6 authors at 4 institutions in 2 countries.
Funding
Abstract
The 6-aminoglucosamine ring of the aminoglycoside antibiotic neomycin B (ring II) was conjugated to a 16-mer peptide nucleic acid (PNA) targeting HIV-1 TAR RNA. For this purpose, we prepared the aminoglucosamine monomer 15 and attached it to the protected PNA prior to its cleavage from the solid support. We found that the resulting PNA-aminoglucosamine conjugate is stable under acidic conditions, efficiently taken up by the human cells and fairly distributed in both cytosol and nucleus without endosomal entrapment because cotreatment with endosome-disrupting agent had no effect on its cellular distribution. The conjugate displayed very high target specificity in vitro and strongly inhibited Tat mediated transactivation of HIV-1 LTR transcription in a cell culture system. The unique properties of this new class of PNA conjugate suggest it to be a potential candidate for therapeutic application.
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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.