Related Experiment Video
Updated: May 21, 2026

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
Published on: November 7, 2025
GPR35 as a Novel Therapeutic Target.
A E Mackenzie1, J E Lappin, D L Taylor
1Molecular Pharmacology Group, Institute of Neuroscience and Psychology, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, UK.
G protein-coupled receptors (GPCRs) like GPR35 are targets for drug discovery. New ligands offer insights into GPR35
Area of Science:
- Pharmacology and drug discovery
- Molecular and cellular biology
- Receptor pharmacology
Background:
- G protein-coupled receptors (GPCRs) are crucial drug targets, yet many remain poorly understood.
- GPR35, a GPCR discovered over a decade ago, has been an "orphan" receptor with undefined endogenous ligands.
- Recent research has identified novel ligands for GPR35, sparking interest in its therapeutic potential.
Purpose of the Study:
- To explore the characterization of the GPR35 receptor.
- To investigate the role of GPR35 in various diseases.
- To identify novel agonist and antagonist ligands for GPR35 to determine its physiological relevance.
Main Methods:
- Review of recent publications on GPR35.
- Analysis of identified endogenous and synthetic ligands.
- Assessment of species-selective properties of ligands.
- Evaluation of GPR35's role in disease models (in vitro and in vivo).
Main Results:
- Novel potent ligands (endogenous and synthetic) for GPR35 have been identified.
- Evidence suggests GPR35 involvement in diseases such as diabetes, hypertension, and asthma.
- Identified ligands exhibit significant species-selective properties, posing drug development challenges.
Conclusions:
- GPR35 is emerging as a promising therapeutic target for various diseases.
- Further research is needed to fully elucidate GPR35's physiological roles and overcome drug development hurdles.
- Identifying novel ligands is key to translating GPR35 research from in vitro and animal models to human applications.
More Related Videos
08:21Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
06:56A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
Published on: March 10, 2018
Related Concept Videos
G Protein-coupled Receptors
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 Receptors
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: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...
Pharmacogenomics: Identification of New Drug Targets
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
GPCR Desensitization