ArticleFrontiers in chemistry2022
Fluorescent Ligand-Based Discovery of Small-Molecule Sulfonamide Agonists for GPR120.
Article in Frontiers in chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed, 6 citations in OpenAlex.
- A Sulfonamide Intermediate Elicits Therapeutic Effect Against Sepsis by Enhancing Neutrophil Maturation.Journal of cellular and molecular medicine · 2026Article
- Potential Therapeutic Exploitation of G Protein-Coupled Receptor 120 (GPR120/FFAR4) Signaling in Obesity-Related Metabolic Disorders.International journal of molecular sciences · 2025Review
- An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism.Nature communications · 2023Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
As a critical member of G protein-coupled receptors (GPCRs), G protein-coupled receptor 120 (GPR120) is a potential target for many physiological diseases, such as type 2 diabetes mellitus, inflammation, and obesity. Considering that small-molecule fluorescent ligands can combine the advantages of visualization, high sensitivity and selectivity, we initially undertook an effort to develop a series of fluorescent ligands to track GPR120 and establish a method to screen GPR120 agonists. The representative fluorescent ligand N1 possesses suitable optical property, equitable biological activity, and high fluorescence imaging feasibility, therefore, based on compound N1, we subsequently founded a bioluminescence resonance energy transfer (BRET) competition binding assay to screen three series of sulfonamide GPR120 agonists we developed herein. The activity evaluation results revealed that compound D5 was a potent GPR120 agonist with high activity and selectivity. Moreover, compound D5 exhibited a significant glucose-lowering effect in db/db mice, which indicates its potential application in the treatment of type 2 diabetes mellitus
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