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Related Experiment Video

Updated: Jun 15, 2026

Gramicidin-based Fluorescence Assay; for Determining Small Molecules Potential for Modifying Lipid Bilayer Properties
10:52

Gramicidin-based Fluorescence Assay; for Determining Small Molecules Potential for Modifying Lipid Bilayer Properties

Published on: October 13, 2010

Screening for small molecules' bilayer-modifying potential using a gramicidin-based fluorescence assay.

Helgi I Ingólfsson1, Olaf S Andersen

  • 1Cornell/Rockefeller/Sloan-Kettering Tri-Institutional Program in Computational Biology and Medicine, New York, New York, USA.

Assay and Drug Development Technologies
|March 18, 2010
PubMed
Summary

Small molecules can alter cell membrane properties, impacting protein function and causing drug side effects. A new gramicidin-based fluorescence assay detects these bilayer-altering compounds for safety screening.

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Area of Science:

  • Biophysics
  • Pharmacology
  • Membrane Biology

Background:

  • Amphiphilic drugs and molecules interact with lipid bilayers, altering their properties.
  • Membrane proteins are sensitive to bilayer changes due to hydrophobic interactions, potentially leading to off-target drug effects.
  • Linear gramicidin channels serve as effective probes for assessing bilayer property alterations experienced by membrane proteins.

Purpose of the Study:

  • To develop a novel gramicidin-based fluorescence assay for quantifying changes in lipid bilayer properties.
  • To establish a scalable method for identifying bilayer-perturbing compounds and potential off-target drug effects.
  • To validate the assay using known bilayer-active compounds like capsaicin.

Main Methods:

  • Utilized large unilamellar vesicles loaded with fluorophores.

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Last Updated: Jun 15, 2026

Gramicidin-based Fluorescence Assay; for Determining Small Molecules Potential for Modifying Lipid Bilayer Properties
10:52

Gramicidin-based Fluorescence Assay; for Determining Small Molecules Potential for Modifying Lipid Bilayer Properties

Published on: October 13, 2010

A Fluorescent Screening Assay for Identifying Modulators of GIRK Channels
05:31

A Fluorescent Screening Assay for Identifying Modulators of GIRK Channels

Published on: April 24, 2012

Automated Lipid Bilayer Membrane Formation Using a Polydimethylsiloxane Thin Film
08:23

Automated Lipid Bilayer Membrane Formation Using a Polydimethylsiloxane Thin Film

Published on: July 10, 2016

  • Measured time-resolved fluorescence quenching kinetics upon the entry of a gramicidin channel-permeable quencher.
  • Employed gramicidin channels as sensors integrated within the lipid bilayer.

    • Main Results:

    • Successfully developed and validated a gramicidin-based fluorescence assay.
    • Demonstrated the assay's capability to detect bilayer property changes induced by compounds such as capsaicin.
    • Showcased the assay's suitability for both detailed mechanistic investigations and high-throughput screening.

    Conclusions:

    • The developed fluorescence assay provides a robust tool for studying drug-induced alterations in lipid bilayer properties.
    • This method can identify compounds that perturb membrane structure and function, offering a strategy to predict and mitigate off-target drug effects.
    • The assay is amenable to high-throughput screening, facilitating the discovery of safer drug candidates.