Related Experiment Video

Updated: Aug 21, 2026

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
09:21

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

Published on: November 7, 2025

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

Christina Bjenning1, Hussien Al-Shamma, William Thomsen

  • 1Division of Metabolic Research, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. CBjenning@arenapharm.com

Current Opinion in Investigational Drugs (London, England : 2000)
|November 13, 2004
PubMed

Insights

New drugs targeting G protein-coupled receptors (GPCRs) are needed to combat rising obesity and type 2 diabetes. Research into both known and orphan GPCRs offers promising therapeutic avenues for these interconnected metabolic disorders.

Area of Science:

  • Pharmacology
  • Endocrinology
  • Metabolic Disorders

Background:

  • Obesity and type 2 diabetes are increasing globally and are closely linked.
  • Weight loss can decrease type 2 diabetes risk and the need for medication.
  • Current lifestyle interventions are insufficient for many, necessitating novel pharmacological treatments.

Purpose of the Study:

  • To review the potential of G protein-coupled receptors (GPCRs) as drug targets for obesity and type 2 diabetes.
  • To highlight the therapeutic relevance of both known and orphan GPCRs.
  • To address the challenge of identifying functions for orphan GPCRs in drug discovery.

Main Methods:

  • Literature review focusing on GPCRs in the central nervous system and pancreas.
  • Analysis of known and orphan GPCRs involved in regulating feeding and glucose homeostasis.
  • Discussion of challenges and opportunities in targeting GPCRs for metabolic diseases.

Main Results:

  • GPCRs in the brain and pancreas are implicated in the regulation of obesity and type 2 diabetes.
  • Orphan GPCRs represent a significant, largely untapped resource for novel drug development.
  • Identifying the function of orphan GPCRs is crucial for next-generation therapeutics.

Conclusions:

  • Known and orphan GPCRs hold substantial potential for developing new drugs to treat obesity and type 2 diabetes.
  • Targeting these receptors could lead to more effective treatments for these prevalent metabolic conditions.
  • Further research into orphan GPCRs is essential for pharmaceutical innovation in metabolic disease therapy.

More Related Videos

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...