ArticleCellular and molecular life sciences : CMLS2014
The stoichiometry of peptide-heparan sulfate binding as a determinant of uptake efficiency of cell-penetrating peptides.
Article in Cellular and molecular life sciences : CMLS, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 53 citations in OpenAlex.
- Hydrophobic and Polarized Aromatic Residues Promote Internalization of Arg-Rich Cell-Penetrating Peptides through Ionpair-π Interactions.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Antiviral efficacy of heparan sulfate and enoxaparin sodium against SARS-CoV-2.Archiv der Pharmazie · 2025Article
- Biological Properties of Arginine-rich Peptides and their Application in Cargo Delivery to Cancer.Current drug delivery · 2025Review
- Deciphering Structural Determinants Distinguishing Active from Inactive Cell-Penetrating Peptides for Cytosolic mRNA Delivery.Bioconjugate chemistry · 2023Article
- Heparan Sulfate and Enoxaparin Interact at the Interface of the Spike Protein of HCoV-229E but Not with HCoV-OC43.Viruses · 2023Article
- Peptides as Pharmacological Carriers to the Brain: Promises, Shortcomings and Challenges.Molecular pharmaceutics · 2022Review
- Designed Multifunctional Peptides for Intracellular Targets.Antibiotics (Basel, Switzerland) · 2022Review
- Membrane Internalization Mechanisms and Design Strategies of Arginine-Rich Cell-Penetrating Peptides.International journal of molecular sciences · 2022Review
- Delivery of antisense oligonucleotides for splice-correction of androgen receptor pre-mRNA in castration-resistant prostate cancer models using cell-penetrating peptides.The Prostate · 2022Article
- Fluid-Phase Endocytosis and Lysosomal Degradation of Bovine Lactoferrin in Lung Cells.Pharmaceutics · 2022Article
- A comparison of acyl-moieties for noncovalent functionalization of PLGA and PEG-PLGA nanoparticles with a cell-penetrating peptide.RSC advances · 2021Article
- Nanotheranostics through Mitochondria-targeted Delivery with Fluorescent Peptidomimetic Nanohybrids for Apoptosis Induction of Brain Cancer Cells.Nanotheranostics · 2021Article
- Glycan-dependent cell adhesion mechanism of Tc toxins.Nature communications · 2020Article
- Understanding Cell Penetration of Cyclic Peptides.Chemical reviews · 2019Review
- Delivery of pDNA Polyplexes to Bronchial and Alveolar Epithelial Cells Using a Mesh Nebulizer.Pharmaceutical research · 2018Article
- Characterisation of neuroprotective efficacy of modified poly-arginine-9 (R9) peptides using a neuronal glutamic acid excitotoxicity model.Molecular and cellular biochemistry · 2017Article
- Vaccine delivery by penetratin: mechanism of antigen presentation by dendritic cells.Immunologic research · 2016Article
- Identification of a Short Cell-Penetrating Peptide from Bovine Lactoferricin for Intracellular Delivery of DNA in Human A549 Cells.PloS one · 2016Article
- Spontaneous membrane-translocating peptides: influence of peptide self-aggregation and cargo polarity.Scientific reports · 2015Article
- Cell-Penetrating Ability of Peptide Hormones: Key Role of Glycosaminoglycans Clustering.International journal of molecular sciences · 2015Article
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Binding to negatively charged heparan sulfates (HS) at the cell surface is considered the first step in the internalization of cationic cell-penetrating peptides (CPPs). However, little is known about the relation of the characteristics of the HS-CPP interaction such as affinity, stoichiometry, and clustering with uptake. In this study, we investigated a collection of mutants of a cyclic CPP derived from human lactoferrin with respect to HS binding and uptake. The thermodynamic parameters of HS binding were determined by isothermal titration calorimetry, clustering of HS was investigated by dynamic light scattering, and cellular uptake by flow cytometry and confocal microscopy. Whereas mutations of non-arginine amino acids that are conserved across lactoferrins of different mammalia only had a minor effect on uptake efficiency, changes in the number of arginine residues influenced the uptake significantly. In general, introduction of arginine residues and cyclization improved the HS affinity and the ability to cluster HS. In particular, there was a strong negative correlation between stoichiometry and uptake, indicating that crosslinking of HS is the driving force for the uptake of arginine-rich CPPs. Using glycan microarrays presenting a collection of synthetic HS, we show that a minimal chain length of HS is required for peptide binding.
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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.