Related Experiment Video
Updated: Oct 1, 2025

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
Physiological relevance of proton-activated GPCRs
Pedro H Imenez Silva1,2, Carsten A Wagner3,4
1Institute of Physiology, University of Zurich, Winterthurerstrasse 190, CH-8057, Zurich, Switzerland. pedrohenrique.imenezsilva@uzh.ch.
This review covers proton-activated G protein-coupled receptors (GPCRs) like GPR4, TDAG8, and OGR1, which sense extracellular pH changes. These receptors play key roles in physiological functions and are implicated in various diseases, offering potential therapeutic targets.
Area of Science:
- Physiology
- Molecular Biology
- Pharmacology
Background:
- Extracellular pH variations are detected by specialized pH-sensing mechanisms.
- Proton-activated G protein-coupled receptors (GPCRs) GPR4, TDAG8, and OGR1 are key players in sensing extracellular pH.
- These receptors are activated by physiological pH changes between 7.5 and 6.5.
Purpose of the Study:
- To review the role of GPR4, TDAG8, and OGR1 in physiological processes.
- To discuss the implications of these receptors in disease pathogenesis.
- To highlight these receptors as potential therapeutic targets.
Main Methods:
- Literature review of studies on GPR4, TDAG8, and OGR1.
- Analysis of receptor expression patterns in different cell types.
- Examination of documented physiological and pathological roles.
Main Results:
- GPR4 and OGR1 are widely expressed, particularly in endothelial and vascular smooth muscle cells.
- TDAG8 expression is mainly found in immune cells.
- These receptors are involved in respiration control, renal adaptation, insulin secretion, mechanosensation, and chemotaxis.
Conclusions:
- GPR4, TDAG8, and OGR1 are crucial for various physiological functions.
- Dysregulation of these receptors is linked to inflammatory diseases and cancer.
- Targeting these pH-sensing GPCRs offers promising therapeutic avenues.
More Related Videos
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
09:12G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
Published on: September 10, 2016
Related Concept Videos
G-Protein Gated Ion Channels
Sensory...
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,...
GPCRs Regulate Adenylyl Cylase Activity
Activation and Inactivation of G Proteins
GPCR Desensitization