Abstract
The roles of G-protein-coupled receptors (GPCRs) in the control of food intake and energy expenditure are being increasingly recognized, and new drug candidates targeting these receptors are making their entry into the clinic. GPCRs exert their action along the various sites of regulation of energy homeostasis control including the central nervous system, the pancreas, the gut and fat cells. Exciting new data about GPCRs recognizing and mediating the effects of lipid mediators and concerning receptors for which no endogenous ligands have been identified yet open new exciting avenues for the validation of additional drug targets. In addition, recently developed paradigms around the concepts of cross-talk regulation and functional selectivity should lead to the development of drugs with improved therapeutic efficacy and reduced undesirable effects. Some of these promising discoveries are discussed in the present article and accompanying papers.
This is a preview of subscription content, access via your institution
Access options
Subscribe to this journal
We are sorry, but there is no personal subscription option available for your country.
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
References
Pierce KL, Premont RT, Lefkowitz RJ . Seven-transmembrane receptors. Nat Rev Mol Cell Biol 2002; 3: 639–650.
Nguyen CA, Akiba Y, Kaunitz JD . Recent advances in gut nutrient chemosensing. Curr Med Chem 2012; 19: 28–34.
Roelofsen H, Priebe MG, Vonk RJ . The interaction of short-chain fatty acids with adipose tissue: relevance for prevention of type 2 diabetes. Benef Microbes 2010; 1: 433–437.
Miller KJ, Murphy BJ, Pelleymounter MA . Central G-Protein Coupled Receptors (GPCR)s as molecular targets for the treatment of obesity: assets, liabilities and development status. Curr Drug Targets CNS Neurol Disord 2004; 3: 357–377.
Xu YL, Jackson VR, Civelli O . Orphan G protein-coupled receptors and obesity. Eur J Pharmacol 2004; 500: 243–253.
Tahrani AA, Bailey CJ, Del Prato S, Barnett AH . Management of type 2 diabetes: new and future developments in treatment. Lancet 2011; 378: 182–197.
Kaku K . Fasiglifam as a new potential treatment option for patients with type 2 diabetes. Expert Opin Pharmacother 2013; 14: 2591–2600.
Samson SL, Garber A . GLP-1R agonist therapy for diabetes: benefits and potential risks. Curr Opin Endocrinol Diabetes Obes 2013; 20: 87–97.
Audet M, Bouvier M . Restructuring G-protein- coupled receptor activation. Cell 2012; 151: 14–23.
Galandrin S, Oligny-Longpré G, Bouvier M . The evasive nature of drug efficacy: implications for drug discovery. Trends Pharmacol Sci 2007; 28: 423–430.
Rajagopal S, Rajagopal K, Lefkowitz RJ . Teaching old receptors new tricks: biasing seven-transmembrane receptors. Nat Rev Drug Discov 2010; 9: 373–386.
Acknowledgements
This article is published as part of a supplement sponsored by the Université Laval's Research Chair in Obesity in an effort to inform the public on the causes, consequences, treatments and prevention of obesity.
Author information
Authors and Affiliations
Corresponding author
Ethics declarations
Competing interests
The authors declare no conflict of interest.
Rights and permissions
About this article
Cite this article
Bouvier, M. Peripheral actions of GPCRs in energy homeostasis: view from the Chair. Int J Obes Supp 4 (Suppl 1), S3–S4 (2014). https://doi.org/10.1038/ijosup.2014.2
Published:
Issue Date:
DOI: https://doi.org/10.1038/ijosup.2014.2
