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Related Concept Videos

Nucleic acids02:43

Nucleic acids

Nucleic acids are the most important macromolecules for the continuity of life. They carry the cell's genetic blueprint and carry instructions for its functioning.
DNA and RNA
The two main types of nucleic acids are deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). DNA is the genetic material in all living organisms, ranging from single-celled bacteria to multicellular mammals. It is in the nucleus of eukaryotes and in the organelles, chloroplasts, and mitochondria. In prokaryotes, the...

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Updated: May 30, 2026

Kinetic Screening of Nuclease Activity using Nucleic Acid Probes
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Kinetic Screening of Nuclease Activity using Nucleic Acid Probes

Published on: November 1, 2019

Nucleic acid aptamers against proteases.

D M Dupont1, L M Andersen, K A Botkjaer

  • 1Department of Molecular Biology, Aarhus University, Gustav Wieds Vej 10C, 8000 Aarhus C, Denmark. dmd@mb.au.dk

Current Medicinal Chemistry
|August 16, 2011
PubMed
Summary
This summary is machine-generated.

Nucleic acid aptamers offer a promising alternative to small molecules for targeting proteases, demonstrating high specificity and therapeutic potential in various diseases. These aptamers can inhibit protease activity and interactions, with some already in clinical trials.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Proteases are critical targets in numerous diseases, but developing specific inhibitors is challenging.
  • Nucleic acid aptamers present a viable alternative for protease inhibition.
  • Aptamers offer high specificity and affinity for protease targets.

Purpose of the Study:

  • To review literature on nucleic acid aptamers selected against protease targets.
  • To explore aptamer selection mechanisms, protein-aptamer recognition, and protease inhibition.
  • To highlight the advantages of aptamers for pharmacological intervention against proteases.

Main Methods:

  • Literature review focusing on aptamer selection strategies for proteases.
  • Analysis of biochemical mechanisms of aptamer-protein interactions.
  • Examination of aptamer-mediated protease inhibition and regulation.

Main Results:

  • Aptamers can be selected for high specificity (nM KD) and conformation-specific binding (e.g., zymogen vs. active forms).
  • Aptamers can inhibit protease enzymatic activity and functionally important exosite interactions.
  • Several aptamers targeting blood coagulation factors are in clinical trials as anticoagulants.

Conclusions:

  • Nucleic acid aptamers are a promising therapeutic strategy for targeting proteases.
  • Aptamers offer advantages in specificity, affinity, and mechanism of action compared to small molecules.
  • Research in protease-binding aptamers showcases innovative selection strategies and regulatory principles.