ArticleChannels (Austin, Tex.)
2-aminoethyl diphenyl borinate (2-APB) inhibits TRPM7 channels through an intracellular acidification mechanism.
Article in Channels (Austin, Tex.). The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
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Who cites it
59 citing papers in PubMed.
- TRPM7 in Peripheral and Central Immune Cells: Emerging Roles in Neuroinflammation and Neurological Disease.International journal of molecular sciences · 2026Review
- Latrophilin-1-Mediated GCells · 2026Article
- ITPR1 Maintains Mitochondrial Redox Homeostasis to Drive Glioblastoma Progression Through Recruitment and Activation of DRP1.Antioxidants (Basel, Switzerland) · 2026Article
- Pathophysiological significance of the TRPM2 ion channel as a potential target in cancer, neurological disorders, and ischemia/reperfusion injury.Pharmacological research · 2026Review
- Age-related changes in calcium ion influx and efflux capacity of human dermal fibroblasts.Cell communication and signaling : CCS · 2026Article
- Boron in Diet and Medicine: Mechanisms of Delivery and Detection.Pharmaceuticals (Basel, Switzerland) · 2025Review
- 3D-printed PCL scaffolds combined with injectable sodium alginate/magnesium-doped mesoporous bioactive glass nanosphere hydrogel for meniscus regeneration: In vitro, In vivo, and multiomics-based therapeutic analyses.Bioactive materials · 2025Article
- Magnetite Nanodiscs Activate Mechanotransductive Calcium Signaling in Diverse Cell Types.Journal of the American Chemical Society · 2025Article
- ThemBio · 2024Article
- Novel benzoylurea derivative decreases TRPM7 channel function and inhibits cancer cells migration.Channels (Austin, Tex.) · 2024Article
- Role of stretch-activated channels in light-generated action potentials mediated by an intramembrane molecular photoswitch.Journal of translational medicine · 2024Article
- Discovery of selective Orai channel blockers bearing an indazole or a pyrazole scaffold.European journal of medicinal chemistry · 2024Article
- Functional and structural insights into activation of TRPV2 by weak acids.The EMBO journal · 2024Article
- Ca2+ Depletion in the ER Causes Store-Operated Ca2+ Entry via the TRPC6 Channel in Mouse Brown Adipocytes.Physiological research · 2024Article
- Vaping-Dependent Pulmonary Inflammation Is CaInternational journal of molecular sciences · 2024Article
- HSP105 inhibition downregulates store-operated calcium entry and promotes acute UVB-induced tight junction disruption.PloS one · 2024Article
- Use of tetraethylammonium (TEA) and Tris loading for blocking TRPM7 channels in intact cells.Frontiers in pharmacology · 2024Article
- Molecular pharmacology of the onco-TRP channel TRPV6.Channels (Austin, Tex.) · 2023Review
- The calcium channel modulator 2-APB hydrolyzes in physiological buffers and acts as an effective radical scavenger and inhibitor of the NADPH oxidase 2.Redox biology · 2023Article
- Pathophysiological Roles of Transient Receptor Potential (Trp) Channels and Zinc Toxicity in Brain Disease.International journal of molecular sciences · 2023Review
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
2-APB is a widely used compound in ion channel research. It affects numerous channels including inositol 1,4,5-trisphosphate receptors, store-operated calcium channels and TRP channels, TRPV3 and TRPM7 among them. A characteristic property of TRPM7 channels is their sensitivity to intracellular Mg ( 2+) and pH. Using patch clamp electrophysiology we find that in Jurkat T lymphocytes, 100-300 µM extracellular 2-APB reversibly inhibits TRPM7 channels when internal HEPES concentration is low (1 mM). Increasing the concentration to 140 mM abolishes the 2-APB effect. Using single-cell fluorescence pH video imaging, we show that at concentrations of 100 µM and higher, 2-APB potently acidifies the cytoplasm. We conclude that TRPM7 sensitivity to 2-APB is not direct but rather, can be explained by cytoplasmic acidification and a resulting channel inhibition.
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