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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
Fragment library screening and lead characterization using SPR biosensors
1Department of Biochemistry and Organic Chemistry, Uppsala University, Uppsala, Sweden. helena.danielson@biorg.uu.se
Current Topics in Medicinal Chemistry
|November 26, 2009
Summary
Fragment-based drug discovery requires sensitive biophysical techniques. Surface Plasmon Resonance (SPR) biosensors are ideal for detecting weak fragment interactions, advancing early drug discovery.
Area of Science:
- Biophysics
- Drug Discovery
- Biochemistry
Background:
- Early drug discovery has shifted from high throughput screening to fragment libraries.
- This transition necessitates sensitive biophysical techniques for interaction analysis.
- Biosensors utilizing Surface Plasmon Resonance (SPR) detection are well-suited for this evolving landscape.
Purpose of the Study:
- To discuss the limitations of SPR for fragment-based lead discovery.
- To review successful studies employing SPR in fragment-based lead discovery.
- To highlight the impact of fragment-based lead discovery on SPR technique evolution.
Main Methods:
- Review of theoretical and experimental limitations of SPR for fragment detection.
- Analysis of published studies on fragment-based lead discovery using SPR.
- Discussion of SPR's applicability to weak interactions.
Main Results:
- SPR is now capable of detecting weakly interacting fragments, not just large molecules.
- The technique has matured significantly in under 20 years.
- Numerous successful applications in fragment-based lead discovery have been documented.
Conclusions:
- SPR biosensors are a powerful tool for fragment-based lead discovery.
- The advancement of SPR is closely tied to the demands of efficient fragment screening.
- SPR enables sensitive analysis of low-molecular-weight compounds in drug discovery.
