Related Experiment Video
Updated: Jun 1, 2026

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
Tyrphostin analogs are GPR35 agonists
Huayun Deng1, Haibei Hu, Ye Fang
1Biochemical Technologies, Science and Technology Division, Corning Inc., Corning, NY 14831, United States.
Researchers discovered new GPR35 agonists using dynamic mass redistribution assays. These compounds are valuable tools for exploring the biological functions of the G protein-coupled receptor 35 (GPR35).
Area of Science:
- Pharmacology
- Cell Biology
- Biochemistry
Background:
- G protein-coupled receptor 35 (GPR35) is an orphan receptor with limited characterization.
- Understanding GPR35's function requires specific pharmacological tools.
Purpose of the Study:
- To identify novel agonists for the orphan GPR35 receptor.
- To develop chemical probes for investigating GPR35 biology.
Main Methods:
- Dynamic mass redistribution (DMR) assays were utilized for high-throughput screening.
- Assays included receptor internalization, Tango β-arrestin translocation, and ERK phosphorylation for agonist confirmation.
Main Results:
- DMR assays successfully identified tyrphostin analogs as potent GPR35 agonists.
- Subsequent assays confirmed the agonist activity of these tyrphostin compounds.
Conclusions:
- Tyrphostin analogs represent a new class of GPR35 agonists.
- These identified agonists serve as crucial pharmacological tools for future GPR35 research.
More Related Videos
09:21BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
Published on: November 7, 2025
07:41A 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
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Activation and Inactivation of G Proteins
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...