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G Protein-Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus

Darren M Riddy1, Philippe Delerive1, Roger J Summers1

  • 1Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia (D.M.R., R.J.S., P.M.S., C.J.L.); and Institut de Recherches Servier, Pôle d'Innovation Thérapeutique Métabolisme, Suresnes, France (P.D.).

Pharmacological Reviews
|December 14, 2017
PubMed

Insights

G protein-coupled receptors (GPCRs) are key targets for treating type 2 diabetes mellitus (T2DM). Understanding their role in insulin resistance and inflammation can lead to new drug discoveries for metabolic disorders.

Area of Science:

  • Pharmacology
  • Endocrinology
  • Metabolic Disorders

Background:

  • G protein-coupled receptors (GPCRs) are implicated in type 2 diabetes mellitus (T2DM) pathogenesis.
  • GPCRs play roles in insulin resistance, beta-cell dysfunction, and inflammation contributing to T2DM.
  • Obesity-induced T2DM is linked to inflammatory pathways involving GPCRs.

Purpose of the Study:

  • To review current literature on GPCR targets for T2DM drug discovery.
  • To identify well-validated and novel GPCR targets for therapeutic intervention.
  • To emphasize the importance of understanding GPCR pharmacology in disease for developing new treatments.

Main Methods:

  • Literature review of current research on GPCRs in T2DM.
  • Analysis of GPCR roles in insulin resistance, beta-cell function, and inflammation.
  • Identification and summary of established and emerging GPCR drug targets.

Main Results:

  • Several GPCRs are validated targets for T2DM treatment.
  • New and promising GPCR targets for drug discovery have been identified.
  • Understanding receptor function is crucial for therapeutic development.

Conclusions:

  • GPCRs represent significant targets for T2DM pharmacotherapy.
  • Further research into GPCRs will facilitate the development of novel drugs for metabolic disorders.
  • Targeting GPCRs holds promise for treating T2DM and related conditions.

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