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VEGFA Gene Silencing in CXCR4-Expressing Cells via siRNA Delivery by Means of Targeted Peptide Carrier
Anna A Egorova1, Marianna A Maretina1,2, Anton V Kiselev3
1D.O. Ott Research Institute of Obstetrics, Gynecology and Reproductology, Saint-Petersburg, Russia.
Abstract:
Discovery of small interfering RNA as a tool for specific gene inhibition led to the development of new therapeutic strategy for the treatment of cancers. The efficacious delivery of therapeutic siRNAs into the cells is a crucial step in RNA interference (RNAi) application, but it remains challenging. Non-viral vectors can provide specific cellular uptake, stable siRNA complex formation, and intracellular siRNA release. Recently, we evaluated modular peptide carrier L1 bearing CXCR4 targeting ligand for its ability to condense siRNA and facilitate endosomal escape and VEGFA gene silencing in CXCR4-expressing endothelial and glioblastoma cells. The present chapter showcases the ability of L1 targeted peptide carrier to form complexes with siRNA and provide efficient VEGFA gene knockdown. We showed that siRNA delivery by means of L1 peptide carrier can result in significant decrease of VEGFA gene expression in A172 glioblastoma cells and in EA.hy 926 endothelial cells. Also, delivery of anti-VEGFA siRNA/peptide complexes led to significant inhibition of endothelial cell migration. Our results showed that L1 peptide carrier modified with CXCR4 ligand is a promising tool for targeted siRNA delivery into CXCR4-expressing cancer and endothelial cells.
Insights
Targeted delivery of small interfering RNA (siRNA) using a novel peptide carrier effectively silenced VEGFA gene expression in cancer and endothelial cells, inhibiting cell migration.
Area of Science:
- Biotechnology
- Molecular Biology
- Cancer Research
Background:
- Small interfering RNA (siRNA) offers a promising therapeutic strategy for cancer treatment via gene inhibition.
- Efficient and targeted delivery of siRNA into cells remains a significant challenge in RNA interference (RNAi) applications.
- Non-viral vectors are being explored for their potential in cellular uptake, complex formation, and intracellular release of siRNA.
Purpose of the Study:
- To evaluate a modular peptide carrier (L1) functionalized with a CXCR4 targeting ligand for its efficacy in siRNA condensation and delivery.
- To assess the ability of the L1 peptide carrier to facilitate endosomal escape and achieve gene silencing of VEGFA.
- To investigate the potential of targeted siRNA delivery for treating CXCR4-expressing cancers and related cellular processes.
Main Methods:
- Development and characterization of the L1 peptide carrier with a CXCR4 targeting ligand.
- Complexation of siRNA with the L1 peptide carrier to form stable nanoparticles.
- In vitro assessment of siRNA delivery and VEGFA gene knockdown in A172 glioblastoma and EA.hy 926 endothelial cells.
- Evaluation of the effect of anti-VEGFA siRNA/peptide complexes on endothelial cell migration.
Main Results:
- The L1 peptide carrier successfully condensed siRNA, forming stable complexes.
- siRNA delivery via the L1 peptide carrier resulted in significant VEGFA gene knockdown in both glioblastoma and endothelial cells.
- Delivery of anti-VEGFA siRNA/peptide complexes significantly inhibited endothelial cell migration.
- The CXCR4 targeting ligand facilitated specific cellular uptake in relevant cell lines.
Conclusions:
- The L1 peptide carrier, modified with a CXCR4 ligand, demonstrates efficient siRNA condensation and delivery capabilities.
- This targeted peptide carrier shows promise for effective VEGFA gene silencing in CXCR4-expressing cancer and endothelial cells.
- The L1 peptide carrier represents a viable tool for targeted RNA interference-based therapeutics in oncology and vascular biology.
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