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G-protein-coupled receptor heterodimerization: assay technologies to clinical significance

Toby Kent1, Cheryl McAlpine, Sahar Sabetnia

  • 1Department of Molecular Pharmacology, Organon Laboratories Ltd, Newhouse, Scotland, ML1 5SH, UK. T.Kent@organon.co.uk

Current Opinion in Drug Discovery & Development
|September 6, 2007
PubMed

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G Protein-coupled Receptors

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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