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Updated: Jul 13, 2026

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
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Orphan seven transmembrane receptor screening.

M J Wigglesworth1, L A Wolfe, A Wise

  • 1Screening and Compound Profiling, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW Essex, UK. Mark.J.Wigglesworth@gsk.com

Ernst Schering Foundation Symposium Proceedings
|August 21, 2007
PubMed
Summary

Identifying natural ligands for orphan seven transmembrane receptors (7TMRs) is key for drug discovery. This review explores methods to find these ligands, unlocking future therapeutic potential.

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Genomics

Background:

  • Seven transmembrane receptors (7TMRs) are a major drug target class, with over 35% of marketed drugs targeting them.
  • The 7TMR superfamily comprises ~720 genes, with half encoding potential drug targets, yet ~155 remain orphan receptors with unknown ligands.
  • Deorphanizing these receptors is crucial for validating new drug targets and understanding disease associations.

Purpose of the Study:

  • To review methodologies for identifying natural ligands for orphan 7TMRs.
  • To provide case studies exemplifying these ligand identification strategies.
  • To highlight the potential of orphan 7TMRs for future drug discovery.

Main Methods:

  • Experimental screening of small molecule and peptide libraries.

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Last Updated: Jul 13, 2026

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  • Reverse pharmacology approaches.
  • Bioinformatic prediction of candidate ligands.
  • Deorphanization through natural ligand identification.

    • Main Results:

    • Established methodologies for identifying ligands at orphan 7TMRs are presented.
    • Case studies illustrate the successful application of these techniques.
    • The review consolidates knowledge on orphan 7TMR ligand discovery.

    Conclusions:

    • Identifying ligands for orphan 7TMRs is a critical step in drug discovery.
    • Diverse methodologies exist to facilitate the deorphanization of these receptors.
    • Unlocking the potential of orphan 7TMRs promises novel therapeutic avenues.