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Cell surface nucleolin as active bait for nanomedicine in cancer therapy: a promising option
Benedetta Ferrara1, Sabrina Belbekhouche2, Damien Habert1
1Université Paris-Est Creteil, Immunorégulation et Biothérapie, INSERM U955, Hôpital Henri Mondor, F-94010 Créteil, France.
Abstract:
Conventional chemotherapy used against cancer is mostly limited due to their non-targeted nature, affecting normal tissue and causing undesirable toxic effects to the affected tissue. With the aim of improving these treatments both therapeutically and in terms of their safety, numerous studies are currently being carried out using nanoparticles (NPs) as a vector combining tumor targeting and carrying therapeutic tools. In this context, it appears that nucleolin, a molecule over-expressed on the surface of tumor cells, is an interesting therapeutic target. Several ligands, antagonists of nucleolin of various origins, such as AS1411, the F3 peptide and the multivalent pseudopeptide N6L have been developed and studied as therapeutic tools against cancer. Over the last ten years or so, numerous studies have been published demonstrating that these antagonists can be used as tumor targeting agents with NPs from various origins. Focusing on nucleolin ligands, the aim of this article is to review the literature recently published or under experimentation in our research team to evaluate the efficacy and future development of these tools as anti-tumor agents.
Insights
Nanoparticles carrying nucleolin ligands show promise for targeted cancer therapy, improving treatment efficacy and reducing side effects compared to conventional chemotherapy.
Area of Science:
- Oncology
- Nanomedicine
- Molecular Biology
Background:
- Conventional chemotherapy faces limitations due to non-targeted action, causing toxicity to normal tissues.
- Nanoparticles (NPs) are being explored as vectors for targeted drug delivery in cancer treatment.
- Nucleolin, a protein over-expressed on tumor cells, presents a viable therapeutic target.
Purpose of the Study:
- To review recent literature and ongoing research on nucleolin ligands for cancer therapy.
- To evaluate the efficacy and future potential of nucleolin-targeted NPs as anti-tumor agents.
Main Methods:
- Literature review of studies on nucleolin antagonists (AS1411, F3 peptide, N6L) conjugated with NPs.
- Analysis of experimental data from the research team on these targeted agents.
Main Results:
- Nucleolin ligands, when incorporated into NPs, demonstrate potential for targeted tumor delivery.
- These targeted approaches show promise in enhancing therapeutic outcomes and minimizing toxicity.
- Ongoing research indicates a positive trajectory for nucleolin-targeted nanoparticle therapies.
Conclusions:
- Nucleolin-targeted nanoparticles represent a promising strategy to overcome limitations of conventional chemotherapy.
- Further development and clinical investigation are warranted to fully realize the anti-tumor potential of these agents.

