ArticleChemistry & biology2015
Attachment of cell-binding ligands to arginine-rich cell-penetrating peptides enables cytosolic translocation of complexed siRNA.
Article in Chemistry & biology, 2015. 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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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 46 citations in OpenAlex.
- An EGFR-Targeted Fusogenic Tandem Peptide for siRNA Delivery in Glioblastoma.Pharmaceutics · 2026Article
- Small Interfering RNA Carriers for Oncotherapy: A Preclinical Overview.Pharmaceutics · 2025Review
- Article
- Intranasal Delivery of Anti-Apoptotic siRNA Complexed with Fas-Signaling Blocking Peptides Attenuates Cellular Apoptosis in Brain Ischemia.Pharmaceutics · 2024Article
- Cell-Penetrating and Targeted Peptides Delivery Systems as Potential Pharmaceutical Carriers for Enhanced Delivery across the Blood-Brain Barrier (BBB).Pharmaceutics · 2023Review
- Advancing peptide siRNA-carrier designs through L/D-amino acid stereochemical modifications to enhance gene silencing.Molecular therapy. Nucleic acids · 2021Article
- Novel fusion peptide-mediated siRNA delivery using self-assembled nanocomplex.Journal of nanobiotechnology · 2021Article
- Systemic α-synuclein injection triggers selective neuronal pathology as seen in patients with Parkinson's disease.Molecular psychiatry · 2021Article
- Cell-Penetrating Peptides Delivering siRNAs: An Overview.Methods in molecular biology (Clifton, N.J.) · 2021Review
- Peptide carriers to the rescue: overcoming the barriers to siRNA delivery for cancer treatment.Translational research : the journal of laboratory and clinical medicine · 2019Review
- Transportan-derived cell-penetrating peptide delivers siRNA to inhibit replication of influenza virus in vivo.Drug design, development and therapy · 2019Article
- Small Interfering RNA-Mediated Control of Virus Replication in the CNS Is Therapeutic and Enables Natural Immunity to West Nile Virus.Cell host & microbe · 2018Article
- Construction and Biological Evaluation of a Novel Integrin αMolecules (Basel, Switzerland) · 2017Article
- Functional peptides for siRNA delivery.Advanced drug delivery reviews · 2017Review
- Use of single chain antibody derivatives for targeted drug delivery.Molecular medicine (Cambridge, Mass.) · 2016Article
- Silencing CCR2 in Macrophages Alleviates Adipose Tissue Inflammation and the Associated Metabolic Syndrome in Dietary Obese Mice.Molecular therapy. Nucleic acids · 2016Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
Abstract
Cell-penetrating peptides (CPPs), such as nona-arginine (9R), poorly translocate siRNA into cells. Our studies demonstrate that attaching 9R to ligands that bind cell surface receptors quantitatively increases siRNA uptake and importantly, allows functional delivery of complexed siRNA. The mechanism involved accumulation of ligand-9R:siRNA microparticles on the cell membrane, which induced transient membrane inversion at the site of ligand-9R binding and rapid siRNA translocation into the cytoplasm. siRNA release also occurred late after endocytosis when the ligand was attached to the L isoform of 9R, but not the protease-resistant 9DR, prolonging mRNA knockdown. This critically depended on endosomal proteolytic activity, implying that partial CPP degradation is required for endosome-to-cytosol translocation. The data demonstrate that ligand attachment renders simple polycationic CPPs effective for siRNA delivery by restoring their intrinsic property of translocation.
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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.