ArticleScientific reports2018
Structure-Activity Investigations and Optimisations of Non-metabolite Agonists for the Succinate Receptor 1.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed.
- Necrotizing enterocolitis is exacerbated through SUCNR1/HIF-1α/BNIP3 axis-mediated succinate-induced intestinal epithelial cell apoptosis.Pediatric research · 2026Article
- Sensing succinate: SUCNR1 as a context-dependent metabolic and cellular signal integrator.Frontiers in molecular biosciences · 2026Review
- Succinate receptor 1 signaling mutually depends on subcellular localization and cellular metabolism.The FEBS journal · 2025Article
- Roles of sensory receptors in non-sensory organs: the kidney and beyond.Nature reviews. Nephrology · 2025Review
- Molecular basis of ligand recognition and activation of the human succinate receptor SUCR1.Cell research · 2024Article
- Cellular succinate metabolism and signaling in inflammation: implications for therapeutic intervention.Frontiers in immunology · 2024Review
- Development and Characterization of Potent Succinate Receptor Fluorescent Tracers.Journal of medicinal chemistry · 2023Article
- Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists.Journal of medicinal chemistry · 2023Article
- Succinate Mediates Tumorigenic EffectsFrontiers in endocrinology · 2021Article
- Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators.Journal of medicinal chemistry · 2020Article
- Gut microbiota-derived succinate: Friend or foe in human metabolic diseases?Reviews in endocrine & metabolic disorders · 2019Review
- Molecular Plasticity of the Nucleus Accumbens Revisited-Astrocytic Waves Shall Rise.Molecular neurobiology · 2019Review
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
The succinate receptor 1 (SUCNR1) is a receptor for the metabolite succinate, which functions as a metabolic stress signal in the liver, kidney, adipose tissue and the retina. However, potent non-metabolite tool compounds are needed to reveal the physiological role and pharmacological potential of SUCNR1. Recently, we published the discovery of a computationally receptor-structure derived non-metabolite SUCNR1 agonist series with high target selectivity. We here report our structure-activity exploration and optimisation that has resulted in the development of agonists with nanomolar potency and excellent solubility and stability properties in a number of in vitro assays. Ligand-guided receptor models with high discriminative power between binding of active and inactive compounds were developed for design of novel chemotypes.
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Registered trials
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