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Islet G-protein coupled receptors: therapeutic potential for diabetes

Shanta J Persaud1

  • 1Diabetes Research Group, Division of Diabetes & Nutritional Sciences, King's College London, UK.

Current Opinion in Pharmacology
|August 21, 2017
PubMed

Insights

Type 2 diabetes (T2D) treatments need new options. Targeting G-protein-coupled receptors (GPCRs) on human islets offers a promising avenue for novel T2D therapies beyond the current GLP-1 receptor agonists.

Area of Science:

  • Endocrinology
  • Pharmacology
  • Metabolic Diseases

Background:

  • Type 2 diabetes (T2D) incidence is rising globally, creating significant healthcare and economic challenges.
  • Existing T2D pharmacotherapies are insufficient, necessitating the exploration of novel therapeutic targets.
  • Human pancreatic islets express numerous G-protein-coupled receptors (GPCRs) with potential for T2D treatment.

Purpose of the Study:

  • To review pharmaceutical development targeting individual or multiple beta-cell GPCRs for T2D.
  • To discuss how understanding GPCR expression in human islets can guide the identification of new therapeutic targets.

Main Methods:

  • Literature review of current pharmaceutical development for GPCR-targeted T2D therapies.
  • Analysis of published data on GPCR expression profiles in human pancreatic islets.

Main Results:

  • The glucagon-like peptide-1 (GLP-1) receptor is the sole islet GPCR with clinically approved agonists for T2D.
  • Exploration of other islet GPCRs represents a significant opportunity for developing new T2D treatments.
  • Targeting multiple GPCRs may offer synergistic therapeutic benefits.

Conclusions:

  • Activating beta-cell GPCRs presents a viable strategy for novel T2D drug development.
  • Comprehensive knowledge of islet GPCR expression is crucial for identifying and prioritizing new drug targets.
  • Further research into GPCR modulation holds promise for addressing the growing T2D epidemic.

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