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Related Experiment Videos

Functional GPCR microarrays.

Yulong Hong1, Brian L Webb, Hui Su

  • 1Science and Technology Division, Corning Inc., Corning, NY 14831, USA.

Journal of the American Chemical Society
|November 3, 2005
PubMed
Summary
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This study presents G-protein-coupled receptor (GPCR) microarrays for drug discovery. These microarrays enable functional assays, streamlining screening for receptor agonists and antagonists.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Materials Science

Background:

  • G-protein-coupled receptors (GPCRs) are crucial drug targets.
  • Developing efficient screening methods for GPCRs is essential for drug discovery.
  • Existing assays may not always integrate primary screening with selectivity and safety assessments.

Purpose of the Study:

  • To describe the development of G-protein-coupled receptor (GPCR) microarrays on porous glass substrates.
  • To demonstrate functional assays for receptor activity using these microarrays.
  • To evaluate the potential of these microarrays in streamlining drug discovery processes.

Main Methods:

  • Fabrication of porous glass slides coated with gamma-aminopropyl silane (GAPS).
  • Creation of GPCR microarrays (neurotensin receptor 1, cholinergic receptor muscarinic 2, opioid receptor mu, cannabinoid receptor 1) via pin printing.

Related Experiment Videos

  • Functional assays utilizing a europium-labeled GTP analogue and a time-gated intensified CCD detector for fluorescence capture.

    • Main Results:

    • Successful fabrication and characterization of GPCR microarrays.
    • Demonstration of selective agonism for each immobilized receptor.
    • Effective screening of potential antagonists using an agonist cocktail.
    • Quantification of receptor activation sufficient for EC50 and IC50 determinations.

    Conclusions:

    • GPCR microarrays on porous glass are a viable platform for functional assays.
    • This technology can integrate primary screening with selectivity and safety evaluations.
    • The developed microarrays offer a streamlined approach to drug discovery without compromising functional information.