ArticleScientific reports2016
2-Aminoethoxydiphenyl Borate Potentiates CRAC Current by Directly Dilating the Pore of Open Orai1.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 23 citations in OpenAlex.
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- Structure and function of the calcium-selective TRP channel TRPV6.The Journal of physiology · 2021Review
- Development of Store-Operated Calcium Entry-Targeted Compounds in Cancer.Frontiers in pharmacology · 2021Review
- Synthesis and Pharmacological Characterization of 2-Aminoethyl Diphenylborinate (2-APB) Derivatives for Inhibition of Store-Operated Calcium Entry (SOCE) in MDA-MB-231 Breast Cancer Cells.International journal of molecular sciences · 2020Article
- The Number and Position of Orai3 Units within Heteromeric Store-Operated CaInternational journal of molecular sciences · 2020Article
- Pacemaker function and neural responsiveness of subserosal interstitial cells of Cajal in the mouse colon.The Journal of physiology · 2020Article
- CaThe Journal of physiology · 2019Article
- Structural bases of TRP channel TRPV6 allosteric modulation by 2-APB.Nature communications · 2018Article
- SOCE mediated by STIM and Orai is essential for pacemaker activity in the interstitial cells of Cajal in the gastrointestinal tract.Science signaling · 2018Article
- Entropy and Polarity Control the Partition and Transportation of Drug-like Molecules in Biological Membrane.Scientific reports · 2017Article
- Polychlorinated biphenyl 19 blocks the most common form of store-operated CaNaunyn-Schmiedeberg's archives of pharmacology · 2017Article
- CRAC channel gating and its modulation by STIM1 and 2-aminoethoxydiphenyl borate.The Journal of physiology · 2017Article
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
2-Aminoethoxydiphenyl borate (2-APB) elicits potentiation current (Ip) on Ca(2+) release-activated Ca(2+) (CRAC) channels. An accurate investigation into this modulation mechanism would reveal how STIM1-dependent channel gating is enhanced, and benefit the future immune enhancer development. Here, we directly probed the pore diameter of CRAC channels and found that 2-APB enlarged the pore size of STIM1-activated Orai1 from 3.8 to 4.6 Å. We demonstrated that ions with small sizes, i.e., Ca(2+) and Na(+), mediated prominent 2-APB-induced Ip on the wildtype (WT) Orai1 channels of narrow pore sizes, while conducted decreased or no Ip on Orai1-V102C/A/G mutant channels with enlarged pore diameters. On the contrary, large Cs(+) ions blocked the WT channels, while displayed large 2-APB induced Ip on pore-enlarged Orai1-V102C/A/G mutant channels, and the potentiation ratio was highest on Orai1-V102C with an intermediate pore size. Furthermore, we showed that 2-APB potentiated Cs(+) current on constitutively active Orai1-V102C/A/G mutants independent of STIM1. Our data suggest that 2-APB directly dilates the pore of open Orai1 channels, both ion size and pore diameter jointly determine the amplitude of Ip on CRAC channels, and the generation of Ip requires the open state of Orai1, not STIM1 itself.
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