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High-Performance Thrombin Aptamers with a Peptide-Extended Recognition Interface
Irina V Varizhuk1, Natalia A Kolganova1, Olga B Gordeeva2,3
1Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 119991 Moscow, Russia.
ACS Omega
|July 24, 2026
Summary
Conjugating peptides to thrombin aptamers enhances their anticoagulant activity and affinity. This peptide-aptamer strategy improves therapeutic potential, though plasma studies reveal potential underestimation of antithrombin effects.
Area of Science:
- Biochemistry
- Molecular Biology
- Biotechnology
Background:
- Aptamers are crucial for diagnostics and therapeutics, but enhancing their affinity and inhibitory properties is key.
- Peptide-aptamer conjugates offer an extended interface to improve aptamer function.
Purpose of the Study:
- To create and evaluate peptide-aptamer conjugates using thrombin aptamers (Re31 and NU172) with a GLE peptide.
- To assess the impact of peptide conjugation on aptamer stability, affinity, and anticoagulant activity.
Main Methods:
- Synthesis of GLE peptide conjugates of Re31 and NU172 thrombin aptamers.
- Biophysical characterization including thermodynamic stability and structural analysis.
- Assessment of anticoagulant activity through thrombin-induced fibrinogen polymerization inhibition and human plasma clotting assays.
Main Results:
- Peptide conjugation did not significantly alter aptamer thermodynamic stability or structure.
- Conjugates exhibited significantly improved affinity and anticoagulant properties compared to unconjugated aptamers.
- The NU172-GLE conjugate demonstrated superior inhibition of thrombin-induced fibrinogen polymerization.
- Antithrombin activity in human plasma may be underestimated due to prothrombin interactions.
Conclusions:
- Peptide-aptamer conjugation is an effective strategy to enhance aptamer affinity and anticoagulant efficacy.
- The NU172-GLE conjugate shows promise as a potent thrombin inhibitor.
- Plasma matrix effects, particularly prothrombin, necessitate careful consideration when evaluating aptamer-based anticoagulants in vivo.
