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Article

2-Aminoethoxydiphenyl borate directly facilitates and indirectly inhibits STIM1-dependent gating of CRAC channels.

The Journal of physiology - 1 Jul 2008

Peinelt Christine, Lis Annette, Beck Andreas, Fleig Andrea, Penner Reinhold

Abstract excerpt

2-Aminoethoxydiphenyl borate (2-APB) has emerged as a useful pharmacological tool in the study of store-operated Ca(2+) entry (SOCE). It has been shown to potentiate store-operated Ca(2+) release-activated Ca(2+) (CRAC) currents at low micromolar concentrations and to inhibit them at higher concentrations. Initial experiments with the three CRAC channel subtypes CRACM1, CRACM2 and CRACM3 have indicated that they...

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Source

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Identifiers

PMID: 18403424
DOI: 10.1113/jphysiol.2008.151365
PMCID: PMC2538778

Genes

STIM1

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

Related research

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Research trail→

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2-Aminoethoxydiphenyl borate directly facilitates and indirectly inhibits STIM1-dependent gating of CRAC channels.PMID 18403424Read ↗

2-Aminoethoxydiphenyl Borate Potentiates CRAC Current by Directly Dilating the Pore of Open Orai1.Semantic proximity Read ↗

2-aminoethoxydiphenyl borate alters selectivity of Orai3 channels by increasing their pore size.Semantic proximity Read ↗

CRACM1, CRACM2, and CRACM3 are store-operated Ca2+ channels with distinct functional properties.Semantic proximity Read ↗

State-dependent block of Orai3 TM1 and TM3 cysteine mutants: insights into 2-APB activation.Semantic proximity Read ↗

The action of selective CRAC channel blockers is affected by the Orai pore geometry.Semantic proximity Read ↗

A single lysine in the N-terminal region of store-operated channels is critical for STIM1-mediated gating.Semantic proximity Read ↗

Review: Structure and Activation Mechanisms of CRAC Channels.Semantic proximity Read ↗

A Ca2(+ )release-activated Ca2(+) (CRAC) modulatory domain (CMD) within STIM1 mediates fast Ca2(+)-dependent inactivation of ORAI1 channels.Semantic proximity Read ↗

Gated regulation of CRAC channel ion selectivity by STIM1.Semantic proximity Read ↗

Inhibition of SERCA Ca2+ pumps by 2-aminoethoxydiphenyl borate (2-APB). 2-APB reduces both Ca2+ binding and phosphoryl transfer from ATP, by interfering with the pathway leading to the Ca2+-binding sites.Semantic proximity Read ↗

CRAC channels and patho-physiology of peripheral organ systems.Semantic proximity Read ↗

Store-dependent and -independent modes regulating Ca2+ release-activated Ca2+ channel activity of human Orai1 and Orai3.Semantic proximity Read ↗

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