ArticleBritish journal of pharmacology2017
Identification and pharmacological characterization of succinate receptor agonists.
Article in British journal of pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 62 citations in OpenAlex.
- Reprogramming of valine metabolism mediated by abnormally low ALDH6A1 expression promotes invasive metastasis of gastric cancer.Science advances · 2026Article
- SUCNR1 coordinates metabolic flux, mitochondrial function, and nutrient-dependent adaptation in hepatocytes.Science advances · 2026Article
- Succinate drives breast cancer bone metastasis by activating the HIF1α/YTHDF1/YAP signaling axis to upregulate chemokine CXCL5 and disrupt the bone microenvironment.Apoptosis : an international journal on programmed cell death · 2026Article
- Mechanisms Involved in Pathological Succinate-Mediated Signaling.International journal of molecular sciences · 2026Review
- Succinate receptor 1 restricts hematopoiesis and prevents acute myeloid leukemia progression.Nature communications · 2026Article
- Elevated methylmalonic acid, but not vitamin B12, predicts all-cause mortality in hyperlipidemic adults: a prospective cohort study.Frontiers in nutrition · 2026Article
- Sensing succinate: SUCNR1 as a context-dependent metabolic and cellular signal integrator.Frontiers in molecular biosciences · 2026Review
- Metabolic toxicity and neurological dysfunction in methylmalonic acidemia: from mechanisms to therapeutics.Molecular medicine (Cambridge, Mass.) · 2025Review
- Succinate receptor 1 signaling mutually depends on subcellular localization and cellular metabolism.The FEBS journal · 2025Article
- Bioassay-Guided Isolation and Identification of Antibacterial Compounds from Invasive Tree of Heaven Stem and Trunk Bark.Molecules (Basel, Switzerland) · 2024Article
- Tuft cell-derived acetylcholine promotes epithelial chloride secretion and intestinal helminth clearance.Immunity · 2024Article
- Untargeted NMR-based metabolomics analysis of kidney allograft perfusates identifies a signature of delayed graft function.Metabolomics : Official journal of the Metabolomic Society · 2024Article
- Methylmalonic acid in aging and disease.Trends in endocrinology and metabolism: TEM · 2024Review
- Type 2 diabetes and succinate: unmasking an age-old molecule.Diabetologia · 2024Review
- Cellular succinate metabolism and signaling in inflammation: implications for therapeutic intervention.Frontiers in immunology · 2024Review
- An evolving view of complex II-noncanonical complexes, megacomplexes, respiration, signaling, and beyond.The Journal of biological chemistry · 2023Review
- Tuft cell-derived acetylcholine regulates epithelial fluid secretion.bioRxiv : the preprint server for biology · 2023Article
- Succinate at the Crossroad of Metabolism and Angiogenesis: Roles of SDH, HIF1α and SUCNR1.Biomedicines · 2022Review
- Succinate metabolism in the retinal pigment epithelium uncouples respiration from ATP synthesis.Cell reports · 2022Article
- SUCNR1 Is Expressed in Human Placenta and Mediates Angiogenesis: Significance in Gestational Diabetes.International journal of molecular sciences · 2021Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe succinate receptor (formerly GPR91 or SUCNR1) is described as a metabolic sensor that may be involved in homeostasis. Notwithstanding its implication in important (patho)physiological processes, the function of succinate receptors has remained ill-defined because no pharmacological tools were available. We report on the discovery of the first family of potent synthetic agonists. EXPERIMENTAL APPROACH: We screened a library of succinate analogues and analysed their activity on succinate receptors. Also, we modelled a pharmacophore and a binding site for this receptor. New agonists were identified based on the information provided by these two approaches. Their activity was studied in various bioassays, including measurement of cAMP levels, [Ca KEY
resultsWe identified cis-epoxysuccinic acid and cis-1,2-cyclopropanedicarboxylic acid as agonists with an efficacy similar to that of succinic acid. Interestingly, cis-epoxysuccinic acid was 10- to 20-fold more potent than succinic acid on succinate receptors. For example, cis-epoxysuccinic acid reduced cAMP levels with a pEC CONCLUSIONS AND IMPLICATIONS: We describe new agonists at succinate receptors that should facilitate further research on this understudied receptor.
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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.