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Updated: Jun 21, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

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Recent advances in 7-transmembrane receptor research.

F D King¹, S Wilson

¹SmithKline Beecham Pharmaceuticals, New Frontiers Science Park (North), Third Avenue, Harlow, EssexCM19 5AW, UK. Frank_King-1@sbphrd.com

Current Opinion in Drug Discovery & Development

|August 4, 2009

Summary

Seven-transmembrane (7-TM) receptors are key drug targets. Genomic advances increase potential 7-TM targets, necessitating research into their roles, ligands, and assays for drug discovery.

Area of Science:

Pharmacology and Drug Discovery
Molecular and Cellular Biology
Genomics and Bioinformatics

Background:

Approximately 50% of marketed drugs target cell surface receptors.
Seven-transmembrane (7-TM) receptors constitute the largest family of these cell surface targets.
Genomic technologies have significantly expanded the number of potential 7-TM receptor targets.

Purpose of the Study:

To review recent advances in the identification, classification, structure, and function of 7-TM receptors.
To discuss novel assay methods for studying 7-TM receptors.
To highlight the identification of new ligands for 7-TM receptors.

Main Methods:

Review of recent scientific literature on 7-TM receptors.
Analysis of data from genomic technologies.

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Examination of current assay methodologies and ligand identification strategies.

Main Results:

Genomic advancements present numerous new 7-TM receptor targets for drug discovery.
New insights into the complex structure-function relationships of 7-TM receptors have emerged.
Progress has been made in developing novel assays and identifying new ligands for these receptors.

Conclusions:

Seven-transmembrane receptors remain critical targets in drug discovery.
Ongoing research and technological advancements are crucial for characterizing novel 7-TM targets and developing effective therapeutics.
The integration of genomics, structural biology, and assay development is key to unlocking the therapeutic potential of 7-TM receptors.