ArticleBritish journal of pharmacology2018
Identification of potent and selective small molecule inhibitors of the cation channel TRPM4.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.
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Who cites it
53 citing papers in PubMed.
- Cryo-EM structure of human NaNature communications · 2026Article
- IPbioRxiv : the preprint server for biology · 2026Article
- Structural mechanism of Necrocide 1 activation of human TRPM4 that triggers necrosis by sodium overload.Nature communications · 2026Article
- TRPM4 Couples Mechanical Force to Myogenic Constriction Throughout the Resistance Vasculature.bioRxiv : the preprint server for biology · 2026Article
- Multi-omics and artificial intelligence for precision drug discovery and potential clinical applications.Signal transduction and targeted therapy · 2026Review
- Temperature and intrinsic CaNature structural & molecular biology · 2026Article
- Potent Anthranilic Anilide-Based TRPM4 Channel Inhibitors Identified by a Structure-Activity Relationship Study.Journal of medicinal chemistry · 2026Article
- Structural mechanism of Necrocide 1 activation of human TRPM4 that triggers necrosis by sodium overload.bioRxiv : the preprint server for biology · 2026Article
- High-Throughput Methods for Variant Functional Assessment in Cardiac Disease.Circulation. Genomic and precision medicine · 2026Review
- Noncanonical calcium-independent TRPM4 activation governs intestinal fluid homeostasis.Nature communications · 2026Article
- Structural biology of the TRPM4 channel: architecture, modulation, and therapeutic opportunities.Frontiers in pharmacology · 2026Review
- Physiological functions and pharmacological targeting of transient receptor potential channels.Pharmacological reviews · 2025Review
- A comprehensive review on the role of acetamido as a linker for the design and discovery of anticancer agents.Medical oncology (Northwood, London, England) · 2025Review
- The TRP channels serving as chemical-to-electrical signal converter.Physiological reviews · 2025Review
- TRPM4 contributes to cell death in prostate cancer tumor spheroids, and to extravasation and metastasis in a zebrafish xenograft model system.Molecular oncology · 2025Article
- Transient Receptor Potential Channels in Prostate Cancer: Associations with ERG Fusions and Survival.International journal of molecular sciences · 2025Article
- Transient Receptor Potential Channels in Vascular Mechanotransduction.American journal of hypertension · 2025Review
- Identification of a binding site for small molecule inhibitors targeting human TRPM4.Nature communications · 2025Article
- The nonsteroidal anti-inflammatory drug meclofenamate mitigates kainic acid-induced seizures via TRPM4 inhibition.Brain communications · 2025Article
- Identification and development of TRPM4 antagonists to counteract neuronal excitotoxicity.iScience · 2024Article
Corrections and comments
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Authors and funding
14 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeTRPM4 is a calcium-activated non-selective cation channel expressed in many tissues and implicated in several diseases, and has not yet been validated as a therapeutic target due to the lack of potent and selective inhibitors. We sought to discover a novel series of small-molecule inhibitors by combining in silico methods and cell-based screening assay, with sub-micromolar potency and improved selectivity from previously reported TRPM4 inhibitors. EXPERIMENTAL APPROACH: Here, we developed a high throughput screening compatible assay to record TRPM4-mediated Na KEY
resultsA series of halogenated anthranilic amides were identified with TRPM4 inhibitory properties with sub-micromolar potency and adequate selectivity. We also showed for the first time that a naturally occurring variant of TRPM4, which displays loss-of-expression and function, is rescued by the most promising compound 5 identified in this study. CONCLUSIONS AND IMPLICATIONS: The discovery of compound 5, a potent and selective inhibitor of TRPM4 with an additional chemical chaperone feature, revealed new opportunities for studying the role of TRPM4 in human diseases and developing clinical drug candidates.
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