ArticleMolecular pharmacology2014
The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35.
Article in Molecular pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 67 citations in OpenAlex.
- An epithelial GPR35 isoform supports tumor-associated transcriptional and metabolic phenotypes.FEBS letters · 2026Article
- Herbacetin as a natural GPR35 agonist for allergic asthma relief via dual regulation of PI3K/Akt/mTOR and MAPK signaling.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Dietary anthocyanidin pelargonidin activates G protein-coupled receptor 35.The FEBS journal · 2026Article
- Disodium Cromoglycate Attenuates the Depressive-Like Behaviors in Mice by Inhibiting Neuroinflammation.CNS neuroscience & therapeutics · 2026Article
- Structure of the GNature communications · 2025Article
- GPR35-mediated metabolic reprogramming promotes tumorigenesis in digestive cancers.Frontiers in immunology · 2025Review
- From orphan to oncogene: The role of GPR35 in cancer and immune modulation.Cytokine & growth factor reviews · 2024Review
- Mast cell stabilizers: from pathogenic roles to targeting therapies.Frontiers in immunology · 2024Review
- The cryptic role of CXCL17/CXCR8 axis in the pathogenesis of cancers: a review of the latest evidence.Journal of cell communication and signaling · 2023Review
- Recent advances in GPR35 pharmacology; 5-HIAA serotonin metabolite becomes a ligand.Archives of pharmacal research · 2023Review
- GPR35 acts a dual role and therapeutic target in inflammation.Frontiers in immunology · 2023Review
- Insights into divalent cation regulation and GCell discovery · 2022Article
- Mitochondrial remodeling and ischemic protection by G protein-coupled receptor 35 agonists.Science (New York, N.Y.) · 2022Article
- G Protein-Coupled Receptor GPR35 Suppresses Lipid Accumulation in Hepatocytes.ACS pharmacology & translational science · 2021Article
- Disruption of GPR35 Signaling in Bone Marrow-Derived Cells Does Not Influence Vascular Inflammation and Atherosclerosis in Hyperlipidemic Mice.Metabolites · 2021Article
- Functional metabolomics reveal the role of AHR/GPR35 mediated kynurenic acid gradient sensing in chemotherapy-induced intestinal damage.Acta pharmaceutica Sinica. B · 2021Article
- GPR35 in Intestinal Diseases: From Risk Gene to Function.Frontiers in immunology · 2021Review
- Article
- Therapeutic Opportunities and Challenges in Targeting the Orphan G Protein-Coupled Receptor GPR35.ACS pharmacology & translational science · 2020Review
- Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35Biomolecules & therapeutics · 2020Article
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
Lack of high potency agonists has restricted analysis of the G protein-coupled receptor GPR35. Moreover, marked variation in potency and/or affinity of current ligands between human and rodent orthologs of GPR35 has limited their productive use in rodent models of physiology. Based on the reported modest potency of the antiasthma and antiallergic ligands cromolyn disodium and nedocromil sodium, we identified the related compounds lodoxamide and bufrolin as high potency agonists of human GPR35. Unlike previously identified high potency agonists that are highly selective for human GPR35, both lodoxamide and bufrolin displayed equivalent potency at rat GPR35. Further synthetic antiallergic ligands, either sharing features of the standard surrogate agonist zaprinast, or with lodoxamide and bufrolin, were also shown to display agonism at either human or rat GPR35. Because both lodoxamide and bufrolin are symmetric di-acids, their potential mode of binding was explored via mutagenesis based on swapping between the rat and human ortholog nonconserved arginine residues within proximity of a key conserved arginine at position 3.36. Computational modeling and ligand docking predicted the contributions of different arginine residues, other than at 3.36, in human GPR35 for these two ligands and were consistent with selective loss of potency of either bufrolin or lodoxamide at distinct arginine mutants. The computational models also suggested that bufrolin and lodoxamide would display reduced potency at a low-frequency human GPR35 single nucleotide polymorphism. This prediction was confirmed experimentally.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.