ArticleNucleic acids research2020
Targeted delivery and enhanced gene-silencing activity of centrally modified folic acid-siRNA conjugates.
Article in Nucleic acids research, 2020. 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, 52 citations in OpenAlex.
- Functional siRNA Delivery via Jet Nebulization: Proof-of-Concept IL-1ß Silencing in Macrophage-like THP-1 Cells.International journal of molecular sciences · 2026Article
- Model-Assisted Process Optimization for Trivalent Ligand-siRNA Conjugation via CuAAC Click Chemistry.ACS omega · 2025Article
- Small Interfering RNA Carriers for Oncotherapy: A Preclinical Overview.Pharmaceutics · 2025Review
- Biological Evaluation of Molecular Spherical Nucleic Acids: Targeting Tumors via a Hybridization-Based Folate Decoration.ACS omega · 2025Article
- Chemical Modifications in Nucleic Acid Therapeutics.Methods in molecular biology (Clifton, N.J.) · 2025Review
- Non-Viral RNA Delivery During Pregnancy: Opportunities and Challenges.Small (Weinheim an der Bergstrasse, Germany) · 2024Review
- Cholesterol Conjugates of Small Interfering RNA: Linkers and Patterns of Modification.Molecules (Basel, Switzerland) · 2024Article
- Non-terminal conjugation of small interfering RNAs with spermine improves duplex binding and serum stability with position-specific incorporation.RSC advances · 2023Article
- Design of Folate-Containing Liposomal Nucleic Acid Delivery Systems for Antitumor Therapy.Pharmaceutics · 2023Review
- Role of MicroRNAs, Aptamers in Neuroinflammation and Neurodegenerative Disorders.Cellular and molecular neurobiology · 2022Review
- The anti-tumor and renoprotection study of E-[c(RGDfK)Journal of nanobiotechnology · 2022Article
- Multi-Functionalized Heteroduplex Antisense Oligonucleotides for Targeted Intracellular Delivery and Gene Silencing in HeLa Cells.Biomedicines · 2022Article
- Article
- Cancer Selective Target Degradation by Folate-Caged PROTACs.Journal of the American Chemical Society · 2021Article
- Surmounting tumor resistance to metallodrugs by co-loading a metal complex and siRNA in nanoparticles.Chemical science · 2021Article
- Chemical strategies for strand selection in short-interfering RNAs.RSC advances · 2021Review
- Article
- Cellular Targeting of Oligonucleotides by Conjugation with Small Molecules.Molecules (Basel, Switzerland) · 2020Review
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
One of the major hurdles in RNAi research has been the development of safe and effective delivery systems for siRNAs. Although various chemical modifications have been proposed to improve their pharmacokinetic behaviour, their delivery to target cells and tissues presents many challenges. In this work, we implemented a receptor-targeting strategy to selectively deliver siRNAs to cancer cells using folic acid as a ligand. Folic acid is capable of binding to cell-surface folate receptors with high affinity. These receptors have become important molecular targets for cancer research as they are overexpressed in numerous cancers despite being expressed at low levels in normal tissues. Employing a post-column copper-catalyzed alkyne-azide cycloaddition (CuAAC), we report the synthesis of siRNAs bearing folic acid modifications at different positions within the sense strand. In the absence of a transfection carrier, these siRNAs were selectively taken up by cancer cells expressing folate receptors. We show that centrally modified folic acid-siRNAs display enhanced gene-silencing activity against an exogenous gene target (∼80% knockdown after 0.75 μM treatment) and low cytotoxicity. In addition, these siRNAs achieved potent dose-dependent knockdown of endogenous Bcl-2, an important anti-apoptotic gene.
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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.