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Related Experiment Video

Updated: Jun 23, 2026

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
07:04

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology

Published on: May 2, 2025

Fragment-based screening using surface plasmon resonance technology.

Samantha Perspicace1, David Banner, Jörg Benz

  • 1F. Hoffmann-La Roche Ltd, Pharma Research, Discovery Technologies, Basel, Switzerland. samantha.perspicace@unibas.ch

Journal of Biomolecular Screening
|May 1, 2009
PubMed
Summary

Surface plasmon resonance (SPR) screening successfully identified 80 potential chymase inhibitors from a library of 2226 small molecules. These fragments bind to distinct regions within the enzyme's active site, validated by X-ray crystallography.

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Area of Science:

  • Biochemistry and structural biology
  • Drug discovery and medicinal chemistry

Background:

  • Surface plasmon resonance (SPR) is a powerful label-free technology for studying molecular interactions.
  • Investigating protein-ligand interactions is crucial for drug discovery and understanding biological processes.

Purpose of the Study:

  • To develop and validate a fragment screening approach using SPR for identifying chymase inhibitors.
  • To characterize the binding of identified fragments to chymase.

Main Methods:

  • Assembled a library of 2226 low-molecular-weight fragments (100-300 Da).
  • Screened fragments for binding to active and zymogen-like chymase using SPR technology.
  • Employed an affinity-selectivity-competition filter cascade for hit identification.
  • Utilized X-ray crystallography to determine the binding modes of selected fragments.

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Multimodal Analytical Platform on a Multiplexed Surface Plasmon Resonance Imaging Chip for the Analysis of Extracellular Vesicle Subsets
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Multimodal Analytical Platform on a Multiplexed Surface Plasmon Resonance Imaging Chip for the Analysis of Extracellular Vesicle Subsets

Published on: March 17, 2023

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Last Updated: Jun 23, 2026

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
07:04

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology

Published on: May 2, 2025

Multimodal Analytical Platform on a Multiplexed Surface Plasmon Resonance Imaging Chip for the Analysis of Extracellular Vesicle Subsets
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Multimodal Analytical Platform on a Multiplexed Surface Plasmon Resonance Imaging Chip for the Analysis of Extracellular Vesicle Subsets

Published on: March 17, 2023

Main Results:

  • Identified 80 positive screening hits with potential binding activity to chymase.
  • Competition experiments indicated that fragments bind to different sites within the chymase active site.
  • X-ray crystallography confirmed the binding of 12 out of 36 co-crystallized fragments within the chymase active site.

Conclusions:

  • The developed SPR-based fragment screening method is effective for identifying enzyme inhibitors.
  • The study validates the utility of the fragment library and SPR as a screening platform.
  • The identified fragments provide starting points for developing novel chymase inhibitors.