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Delivery, Effect on Cell Viability, and Plasticity of Modified Aptamer Constructs
Olof Gissberg1, Eman M Zaghloul1, Karin E Lundin1
11 Department of Laboratory Medicine, Karolinska Institutet, and Karolinska University Hospital , Huddinge, Sweden .
Nucleic Acid Therapeutics
|February 10, 2016
Summary
AS1411 aptamer delivery is influenced by attached oligonucleotide cargo. Modifications to the aptamer and cargo can impact cancer cell uptake and cytotoxicity, offering insights for targeted cancer therapy design.
Area of Science:
- Biochemistry
- Molecular Biology
- Cancer Research
Background:
- AS1411 is a guanine-quadruplex aptamer that targets cancer cells via nucleolin receptors.
- Aptamer-drug conjugates are being explored for targeted cancer therapy.
Purpose of the Study:
- To investigate how different oligonucleotide (ON) cargo and modifications affect AS1411 aptamer cell internalization and function.
- To explore the impact of unlocked nucleic acid (UNA) modifications on AS1411 structure and delivery.
Main Methods:
- Studied AS1411 carrying locked nucleic acid (LNA)-containing ONs in A549 and U2OS cancer cells.
- Assessed cell internalization efficiency and cytotoxicity of modified aptamers.
- Analyzed the secondary structure of AS1411 with cargo and UNA modifications, with and without ellipticine derivatives.
Main Results:
- Internalization efficiency and antitumor activity depend on the ON cargo's chemical properties.
- AS1411 lost its inherent antitumor properties when linked to a non-toxic ON (noTox).
- A toxic ON (Tox) showed potent cytotoxicity upon AS1411-mediated uptake in A549 cells.
Conclusions:
- Cargo chemistry and composition are critical for aptamer-mediated delivery and efficacy.
- UNA modifications and cargo influence AS1411's structural plasticity and delivery capabilities.
- Findings provide insights for designing improved aptamer-guided delivery systems for cancer therapeutics.
