Article ; Online: 2-aminoethyl diphenyl borinate (2-APB) inhibits TRPM7 channels through an intracellular acidification mechanism.
2012 Volume 6, Issue 5, Page(s) 362–369
Abstract: ... among them. A characteristic property of TRPM7 channels is their sensitivity to intracellular Mg ( 2+) and pH. Using patch ... inhibits TRPM7 channels when internal HEPES concentration is low (1 mM). Increasing the concentration ... 2-APB is a widely used compound in ion channel research. It affects numerous channels including ...
| 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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| MeSH term(s) | Boron Compounds/pharmacology ; Humans ; Hydrogen-Ion Concentration ; Ion Channel Gating/drug effects ; Jurkat Cells ; Magnesium/metabolism ; Patch-Clamp Techniques ; Protein-Serine-Threonine Kinases ; TRPM Cation Channels/antagonists & inhibitors ; TRPM Cation Channels/metabolism |
| Chemical Substances | Boron Compounds ; TRPM Cation Channels ; 2-aminoethoxydiphenyl borate (E4ES684O93) ; Protein-Serine-Threonine Kinases (EC 2.7.11.1) ; TRPM7 protein, human (EC 2.7.11.1) ; Magnesium (I38ZP9992A) |
| Language | English |
| Publishing date | 2012-08-24 |
| Publishing country | United States |
| Document type | Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't |
| ZDB-ID | 2262854-X |
| ISSN | 1933-6969 ; 1933-6969 |
| ISSN (online) | 1933-6969 |
| ISSN | 1933-6969 |
| DOI | 10.4161/chan.21628 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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