ArticleScientific reports2017
Tumor-targeted delivery of siRNA using fatty acyl-CGKRK peptide conjugates.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 29 citations in OpenAlex.
- Innovative nanodelivery systems for targeted breast cancer therapy: overcoming drug delivery challenges and exploring future perspectives.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Design, Synthesis, and Evaluation of Oleyl-WRH Peptides for siRNA Delivery.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Chitosan-Based Nanoparticles for Nucleic Acid Delivery: Technological Aspects, Applications, and Future Perspectives.Pharmaceutics · 2023Review
- Amphiphilic Polypeptides Obtained by Post-Polymerization Modification of Poly-l-Lysine as Systems for Combined Delivery of Paclitaxel and siRNA.Pharmaceutics · 2023Article
- Chitosan and Its Structural Modifications for siRNA Delivery.Advanced pharmaceutical bulletin · 2023Review
- Modified Linear Peptides Effectively Silence STAT-3 in Breast Cancer and Ovarian Cancer Cell Lines.Pharmaceutics · 2023Article
- Oleyl Conjugated Histidine-Arginine Cell-Penetrating Peptides as Promising Agents for siRNA Delivery.Pharmaceutics · 2022Article
- Lipids and Lipid Derivatives for RNA Delivery.Chemical reviews · 2021Review
- Cyclic Peptide-Gadolinium Nanocomplexes as siRNA Delivery Tools.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Peptide-Assisted Nucleic Acid Delivery Systems on the Rise.International journal of molecular sciences · 2021Review
- Lauroylated Histidine-Enriched S4Pharmaceutical research · 2020Article
- Synthesis and Antiproliferative Activities of Conjugates of Paclitaxel and Camptothecin with a Cyclic Cell-Penetrating Peptide.Molecules (Basel, Switzerland) · 2019Article
- Au-CGKRK Nanoconjugates for Combating Cancer through T-Cell-Driven Therapeutic RNA Interference.ACS omega · 2018Article
- Design, Synthesis, and Evaluation of Homochiral Peptides Containing Arginine and Histidine as Molecular Transporters.Molecules (Basel, Switzerland) · 2018Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tumor-targeted carriers provide efficient delivery of chemotherapeutic agents to tumor tissue. CGKRK is one of the well-known tumor targeting peptides with significant specificity for angiogenic blood vessels and tumor cells. Here, we designed fatty acyl conjugated CGKRK peptides, based on the hypothesis that hydrophobically-modified CGKRK peptide could enhance cellular permeation and delivery of siRNA targeted to tumor cells for effective silencing of selected proteins. We synthesized six fatty acyl-peptide conjugates, using a diverse chain of saturated and unsaturated fatty acids to study the efficiency of this approach. At peptide:siRNA weight/weight ratio of 10:1 (N/P ≈ 13.6), almost all the peptides showed complete binding with siRNA, and at a w/w ratio of 20:1 (N/P ≈ 27.3), complete protection of siRNA from early enzymatic degradation was observed. Conjugated peptides and peptide/siRNA complexes did not show significant cytotoxicity in selected cell lines. The oleic acid-conjugated peptide showed the highest efficiency in siRNA uptake and silencing of kinesin spindle protein at peptide:siRNA w/w ratio of 80:1 (N/P ≈ 109). The siRNA internalization into non-tumorigenic kidney cells was negligible with all fatty acyl-peptide conjugates. These results indicate that conjugation of fatty acids to CGKRK could create an efficient delivery system for siRNA silencing specifically in tumor cells.
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