Related Experiment Video
Updated: Jun 23, 2026
06:52
Kinetic Screening of Nuclease Activity using Nucleic Acid Probes
Published on: November 1, 2019
Peptide aptamers for small molecule drug discovery
Carine Bardou1, Christophe Borie, Marc Bickle
1Aptanomics S.A., Imaxio, Lyon, France.
Methods in Molecular Biology (Clifton, N.J.)
|April 21, 2009
Summary
Peptide aptamers are valuable tools for drug discovery. A new high-throughput screening assay, AptaScreen, efficiently identifies small molecules that disrupt protein-peptide aptamer interactions, aiding therapeutic target validation.
Area of Science:
- Biotechnology and Drug Discovery
- Molecular Biology and Protein Interactions
Background:
- Peptide aptamers serve as research tools for protein function analysis and regulatory network studies.
- They are increasingly utilized in therapeutic research for target identification, validation, and drug discovery.
- Their combinatorial nature allows interrogation of diverse molecular surfaces on target proteins.
Purpose of the Study:
- To present a high-throughput screening assay for identifying small molecules that displace protein-peptide aptamer interactions.
- To validate peptide aptamers as guides for discovering small molecule drugs targeting specific molecular surfaces.
Main Methods:
- Development of AptaScreen, a duplex yeast two-hybrid assay.
- Incorporation of two luciferase reporter genes for signal detection.
- Assay adaptable to 96- and 384-well plate formats and amenable to full automation.
Main Results:
- The AptaScreen assay successfully identifies small molecules that disrupt protein-peptide aptamer binding.
- Demonstration of a high-throughput screening capability for drug discovery applications.
Conclusions:
- AptaScreen is an efficient method for identifying therapeutic targets and validating drug candidates.
- This assay facilitates the discovery of small molecules that modulate protein function via peptide aptamer interactions.
