ArticleBeilstein journal of organic chemistry2012
Dimerization of a cell-penetrating peptide leads to enhanced cellular uptake and drug delivery.
Article in Beilstein journal of organic chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 58 citations in OpenAlex.
- Antimicrobial and Cell-Penetrating Peptides: Understanding Penetration for the Design of Novel Conjugate Antibiotics.Antibiotics (Basel, Switzerland) · 2022Review
- Redesigning of Cell-Penetrating Peptides to Improve Their Efficacy as a Drug Delivery System.Pharmaceutics · 2022Review
- Anti-Pythium insidiosum activity of MSI-78, LL-37, and magainin-2 antimicrobial peptides.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2022Article
- Cell-penetrating peptides improve pharmacokinetics and pharmacodynamics of anticancer drugs.Tissue barriers · 2022Review
- TAT for Enzyme/Protein Delivery to Restore or Destroy Cell Activity in Human Diseases.Life (Basel, Switzerland) · 2021Review
- Perfluoro-tert-butanol for selective on-resin detritylation: a mild alternative to traditionally used methods.Amino acids · 2021Article
- microRNAs in the Antitumor Immune Response and in Bone Metastasis of Breast Cancer: From Biological Mechanisms to Therapeutics.International journal of molecular sciences · 2020Review
- Comparison of bulk and microfluidics methods for the formulation of poly-lactic-International journal of pharmaceutics: X · 2019Article
- Recent Advances in Cell Penetrating Peptide-Based Anticancer Therapies.Molecules (Basel, Switzerland) · 2019Review
- Peptide and protein nanoparticle conjugates: versatile platforms for biomedical applications.Chemical Society reviews · 2018Review
- Design and biological characterization of novel cell-penetrating peptides preferentially targeting cell nuclei and subnuclear regions.Beilstein journal of organic chemistry · 2018Article
- Dimerization in tailoring uptake efficacy of the HSV-1 derived membranotropic peptide gH625.Scientific reports · 2017Article
- Characterization of a Cell-Penetrating Peptide with Potential Anticancer Activity.ChemMedChem · 2017Article
- Trends in the Binding of Cell Penetrating Peptides to siRNA: A Molecular Docking Study.Journal of biophysics (Hindawi Publishing Corporation : Online) · 2017Article
- Design and Application of Antimicrobial Peptide Conjugates.International journal of molecular sciences · 2016Review
- A Cell-Permeable ATP Analogue for Kinase-Catalyzed Biotinylation.Angewandte Chemie (International ed. in English) · 2015Article
- Protein delivery into live cells by incubation with an endosomolytic agent.Nature methods · 2014Article
- The Human Cathelicidin Antimicrobial Peptide LL-37 as a Potential Treatment for Polymicrobial Infected Wounds.Frontiers in immunology · 2013Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Over the past 20 years, cell-penetrating peptides (CPPs) have gained tremendous interest due to their ability to deliver a variety of therapeutically active molecules that would otherwise be unable to cross the cellular membrane due to their size or hydrophilicity. Recently, we reported on the identification of a novel CPP, sC18, which is derived from the C-terminus of the 18 kDa cationic antimicrobial protein. Furthermore, we demonstrated successful application of sC18 for the delivery of functionalized cyclopentadienyl manganese tricarbonyl (cymantrene) complexes to tumor cell lines, inducing high cellular toxicity. In order to increase the potential of the organometallic complexes to kill tumor cells, we were looking for a way to enhance cellular uptake. Therefore, we designed a branched dimeric variant of sC18, (sC18)(2), which was shown to have a dramatically improved capacity to internalize into various cell lines, even primary cells, using flow cytometry and fluorescence microscopy. Cell viability assays indicated increased cytotoxicity of the dimer presumably caused by membrane leakage; however, this effect turned out to be dependent on the specific cell type. Finally, we could show that conjugation of a functionalized cymantrene with (sC18)(2) leads to significant reduction of its IC(50) value in tumor cells compared to the respective sC18 conjugate, proving that dimerization is a useful method to increase the drug-delivery potential of a cell-penetrating peptide.
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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.