ArticleThe Journal of pharmacology and experimental therapeutics2012
Antagonists of GPR35 display high species ortholog selectivity and varying modes of action.
Article in The Journal of pharmacology and experimental therapeutics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 52 citations in OpenAlex.
- GPR35 Mediates the Proliferation and Adipogenesis of Goat Intramuscular Preadipocytes Through the cAMP/PKA Signaling Pathway.Animals : an open access journal from MDPI · 2026Article
- Cell Signaling by Tryptophan Catabolism.Biochemistry · 2026Review
- Dietary anthocyanidin pelargonidin activates G protein-coupled receptor 35.The FEBS journal · 2026Article
- GPR35 prevents drug-induced liver injury via the Gαs-cAMP-PKA axis in macrophages.Cellular and molecular life sciences : CMLS · 2025Article
- Article
- The power of many: Multilevel targeting of representative chemokine and metabolite GPCRs in personalized cancer therapy.European journal of immunology · 2024Review
- From orphan to oncogene: The role of GPR35 in cancer and immune modulation.Cytokine & growth factor reviews · 2024Review
- Recent advances in GPR35 pharmacology; 5-HIAA serotonin metabolite becomes a ligand.Archives of pharmacal research · 2023Review
- GPR35 antagonist CID-2745687 attenuates anchorage-independent cell growth by inhibiting YAP/TAZ activity in colorectal cancer cells.Frontiers in pharmacology · 2023Article
- GPR35 acts a dual role and therapeutic target in inflammation.Frontiers in immunology · 2023Review
- G Protein-Coupled Receptor GPR35 Suppresses Lipid Accumulation in Hepatocytes.ACS pharmacology & translational science · 2021Article
- G-protein coupled receptor 35 (GPR35) regulates the colonic epithelial cell response to enterotoxigenic Bacteroides fragilis.Communications biology · 2021Article
- GPR35 in Intestinal Diseases: From Risk Gene to Function.Frontiers in immunology · 2021Review
- Therapeutic Opportunities and Challenges in Targeting the Orphan G Protein-Coupled Receptor GPR35.ACS pharmacology & translational science · 2020Review
- Review: Pathogenesis of cholestatic liver diseases.World journal of hepatology · 2020Review
- Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35Biomolecules & therapeutics · 2020Article
- Receptor selectivity between the G proteins GαFASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2019Article
- On-target and off-target effects of novel orthosteric and allosteric activators of GPR84.Scientific reports · 2019Article
- The Orphan Receptor GPR35 Contributes to Angiotensin II-Induced Hypertension and Cardiac Dysfunction in Mice.American journal of hypertension · 2018Article
- Evidence for the Existence of a CXCL17 Receptor Distinct from GPR35.Journal of immunology (Baltimore, Md. : 1950) · 2018Article
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
Variation in pharmacology and function of ligands at species orthologs can be a confounding feature in understanding the biology and role of poorly characterized receptors. Substantial selectivity in potency of a number of GPR35 agonists has previously been demonstrated between human and rat orthologs of this G protein-coupled receptor. Via a bioluminescence resonance energy transfer-based assay of induced interactions between GPR35 and β-arrestin-2, addition of the mouse ortholog to such studies indicated that, as for the rat ortholog, murine GPR35 displayed very low potency for pamoate, whereas potency for the reference GPR35 agonist zaprinast was intermediate between the rat and human orthologs. This pattern was replicated in receptor internalization and G protein activation assays. The effectiveness and mode of action of two recently reported GPR35 antagonists, methyl-5-[(tert-butylcarbamothioylhydrazinylidene)methyl]-1-(2,4-difluorophenyl)pyrazole-4-carboxylate (CID-2745687) and 2-hydroxy-4-[4-(5Z)-5-[(E)-2-methyl-3-phenylprop-2-enylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]butanoylamino)benzoic acid (ML-145), were investigated. Both CID-2745687 and ML-145 competitively inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding site. By contrast, although ML-145 also competitively antagonized the effects of pamoate, CID-2745687 acted in a noncompetitive fashion. Neither ML-145 nor CID-2745687 was able to effectively antagonize the agonist effects of either zaprinast or cromolyn disodium at either rodent ortholog of GPR35. These studies demonstrate that marked species selectivity of ligands at GPR35 is not restricted to agonists and considerable care is required to select appropriate ligands to explore the function of GPR35 in nonhuman cells and tissues.
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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.