G protein-coupled receptors as targets for anti-diabetic therapeutics

Dayoung Oh, Jerrold M. Olefsky

Research output: Contribution to journalReview articlepeer-review

68 Scopus citations


The prevalence of obesity and type 2 diabetes (T2D) is increasing worldwide, and these two metabolic disorders are closely linked. Lifestyle modification, including weight loss and exercise, are effective treatments for T2D, but, unfortunately, most patients are unsuccessful at maintaining durable weight reduction and recidivism is all too common. Therefore, safe and efficacious drugs are required for the successful treatment of T2D in a large proportion of patients. Targeting G protein-coupled receptors (GPCRs) in metabolic tissues-such as adipose tissue, liver, muscle, pancreatic islets, immune cells and the central nervous system-has emerged as a key target for current and future anti-diabetic compounds. This Opinion focuses on the potential of GPCRs as targets for the discovery of new drugs to successfully treat T2D.

Original languageEnglish (US)
Pages (from-to)161-172
Number of pages12
JournalNature Reviews Drug Discovery
Issue number3
StatePublished - Mar 1 2016

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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