ArticleScientific reports2022
Hydrophobicity is a key determinant in the activity of arginine-rich cell penetrating peptides.
Article in Scientific reports, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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
19 citing papers in PubMed, 42 citations in OpenAlex.
- EB1010, a putative Christensenellaceae-derived microbial peptide, exhibits anti-inflammatory activity and therapeutic potential in ulcerative colitis.Gut microbes · 2026Article
- The position of hydrophobic residues impacts cellular uptake and intracellular localization of cell penetrating peptides.RSC chemical biology · 2026Article
- Exploring CPP Enhanced Hypoxia Targeting: An Approach Using Radiolabeled 2-nitroimidazole TAT Conjugate.Drug development research · 2026Article
- Functional Peptide-Based Biomaterials for Pharmaceutical Application: Sequences, Mechanisms, and Optimization Strategies.Journal of functional biomaterials · 2026Review
- Mannose Targeting and Hydrophobic Tuning of Polycationic Vectors for Efficient Immunostimulatory CpG Delivery.ACS applied nano materials · 2025Article
- Peptide-Based Inorganic Nanoparticles as Efficient Intracellular Delivery Systems.Pharmaceutics · 2025Review
- Clickable Pyclen-Based Luminescent Lanthanide Complexes: Application to Two-Photon Microscopy.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Hydrophobic and Polarized Aromatic Residues Promote Internalization of Arg-Rich Cell-Penetrating Peptides through Ionpair-π Interactions.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Peptides: potential delivery systems for mRNA.RSC chemical biology · 2025Review
- An immunoregulatory amphipathic peptide derived from Fasciola hepatica helminth defense molecule (FhHDM-1.C2) exhibits potent biotherapeutic activity in a murine model of multiple sclerosis.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2025Article
- PerseuCPP: a machine learning strategy to predict cell-penetrating peptides and their uptake efficiency.Bioinformatics advances · 2025Article
- Endosomal Escape and Nuclear Localization: Critical Barriers for Therapeutic Nucleic Acids.Molecules (Basel, Switzerland) · 2024Review
- Conditional Cell-Penetrating Peptide Exposure as Selective Nanoparticle Uptake Signal.ACS applied materials & interfaces · 2024Article
- Organ- and Cell-Selective Delivery of mRNA In Vivo Using Guanidinylated Serinol Charge-Altering Releasable Transporters.Journal of the American Chemical Society · 2024Article
- Protein-based nanoparticles for therapeutic nucleic acid delivery.Biomaterials · 2024Review
- Elucidating the Impact of Payload Conjugation on the Cell-Penetrating Efficiency of the Endosomal Escape Peptide dfTAT: Implications for Future Designs for CPP-Based Delivery Systems.Bioconjugate chemistry · 2023Article
- Therapeutic Oligonucleotides: An Outlook on Chemical Strategies to Improve Endosomal Trafficking.Cells · 2023Review
- Delivered complementation in planta (DCIP) enables measurement of peptide-mediated protein delivery efficiency in plants.Communications biology · 2023Article
- Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
To deliver useful biological payloads into the cytosolic space of cells, cell-penetrating peptides have to cross biological membranes. The molecular features that control or enhance this activity remain unclear. Herein, a dimeric template of the arginine-rich HIV TAT CPP was used to establish the effect of incorporating groups and residues of various chemical structures and properties. A positive correlation is established between the relative hydrophobicity of these additional moieties and the ability of the CPP conjugates to deliver a peptidic probe into live cells. CPP conjugates with low hydrophobicity lead to no detectable delivery activity, while CPPs containing groups of increasing hydrophobicity achieve intracellular delivery at low micromolar concentrations. Notably, the chemical structures of the hydrophobic groups do not appear to play a role in overall cell penetration activity. The cell penetration activity detected is consistent with endosomal escape. Leakage assays with lipid bilayer of endosomal membrane composition also establish a positive correlation between hydrophobicity and membrane permeation. Overall, these results indicate that the presence of a relatively hydrophobic moiety, regardless of structure, is required in a CPP structure to enhance its cell penetration. It also indicates that simple modifications, including fluorophores used for cell imaging or small payloads, modulate the activity of CPPs and that a given CPP-conjugate may be unique in its membrane permeation properties.
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