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G protein-coupled receptors as therapeutic targets for obesity and type 2 diabetes.

Abstract
The prevalence of obesity and type 2 diabetes, two strongly correlated disorders, is increasing worldwide. Weight loss can reduce the risk of developing type 2 diabetes and the pharmacological treatments normally required to manage this disorder. Even though dietary and lifestyle changes may eventually reduce obesity for some individuals, new safe and more efficacious drugs are required for successful weight reduction and treatment of type 2 diabetes in a large proportion of obese individuals. In addition to targeting known G protein-coupled receptors (GPCRs), several orphan GPCRs expressed in central nervous system areas known to regulate feeding may provide new targets for the treatment of obesity. Similarly, the pancreas contains numerous islet GPCRs as well as an abundance of orphan GPCRs that potentially could emerge as targets for future antidiabetic compounds. One of the major challenges facing the pharmaceutical industry is how to rapidly establish the function and therapeutic relevance of orphan GPCRs, some of which may represent novel targets for the discovery of the next generation of drugs to effectively treat obesity and type 2 diabetes. This review will focus on the significant potential of known and orphan GPCRs as targets for the discovery of new drugs to successfully treat these serious disorders.
AuthorsChristina Bjenning, Hussien Al-Shamma, William Thomsen, Jim Leonard, Dominic Behan
JournalCurrent opinion in investigational drugs (London, England : 2000) (Curr Opin Investig Drugs) Vol. 5 Issue 10 Pg. 1051-62 (Oct 2004) ISSN: 1472-4472 [Print] England
PMID15535426 (Publication Type: Journal Article, Review)
Chemical References
  • Hypoglycemic Agents
  • Ligands
  • Receptors, G-Protein-Coupled
Topics
  • Animals
  • Appetite Regulation (drug effects)
  • Diabetes Mellitus, Type 2 (drug therapy, metabolism)
  • Energy Metabolism (drug effects)
  • Humans
  • Hypoglycemic Agents (pharmacology, therapeutic use)
  • Ligands
  • Obesity (drug therapy, metabolism)
  • Receptors, G-Protein-Coupled (metabolism)

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