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Mapping the Binding Site of an Aptamer on ATP Using MicroScale Thermophoresis
Published on: January 7, 2017
Entropic fragment-based approach to aptamer design.
Chih-Yuan Tseng1, Md Ashrafuzzaman, Jonathan Y Mane
1Department of Oncology, University of Alberta, Edmonton, AB, Canada. chih-yuan.tseng@ualberta.ca
Chemical Biology & Drug Design
|April 19, 2011
Summary
This study introduces a new theoretical method for designing aptamers, which are DNA/RNA molecules used in diagnostics and therapeutics. The approach uses target structure information to create aptamer templates, improving efficiency and potentially modifying affinity without the standard selection process.
Area of Science:
- Biochemistry
- Molecular Biology
- Bioinformatics
Background:
- Aptamers are short nucleic acid sequences with high specificity for molecular targets.
- Systematic Evolution of Ligands by Exponential Enrichment (SELEX) is the standard method for aptamer discovery.
- SELEX requires significant sequence diversity and structural complexity, and efficient identification of aptamers remains challenging.
Purpose of the Study:
- To propose a novel information-driven approach for theoretical aptamer template design.
- To enable aptamer design based solely on biomolecular target structures.
- To improve the efficiency of aptamer identification and facilitate affinity modification.
Main Methods:
- Developed a theoretical framework for aptamer template design using target structure information.
- Investigated the approach using computational and experimental methods.
- Validated the method with two specific targets: thrombin and phosphatidylserine.
Main Results:
- The proposed information-driven approach demonstrated applicability for theoretical aptamer design.
- Case studies with thrombin and phosphatidylserine supported the method's efficacy.
- The approach allows for modification of designed aptamer sequences to enhance binding affinity.
Conclusions:
- The novel theoretical design approach offers a promising advancement in aptamer development.
- This method can potentially streamline aptamer discovery and optimization.
- It provides an alternative strategy for generating high-affinity aptamers, especially when SELEX is challenging.

