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Article

The action of selective CRAC channel blockers is affected by the Orai pore geometry.

Cell calcium - 1 Feb 2013

Derler Isabella, Schindl Rainer, Fritsch Reinhard, Heftberger Peter, Riedl Maria Christine, Begg Malcolm, House David, Romanin Christoph

Abstract excerpt

As the molecular composition of calcium-release activated calcium (CRAC) channels has been unknown for two decades, elucidation of selective inhibitors has been considerably hampered. By the identification of the two key components of CRAC channels, STIM1 and Orai1 have emerged as promising targets for CRAC blockers. The aim of this study was to thoroughly characterize the effects of two selective CRAC channel...

Topics

Allosteric Regulation
Calcium
Calcium Channel Blockers
Calcium Channels
Calcium Signaling
Fluorescence Resonance Energy Transfer
HEK293 Cells
Humans
Membrane Proteins
Microscopy, Fluorescence

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Mutation

Neoplasm Proteins

ORAI1 Protein

Patch-Clamp Techniques

Protein Binding

Protein Multimerization

Stromal Interaction Molecule 1

Transfection

Source

Open in PubMed Open full text

Identifiers

PMID: 23218667
DOI: 10.1016/j.ceca.2012.11.005
PMCID: PMC3580291

Genes

STIM1

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 31 Aug 2026.

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The action of selective CRAC channel blockers is affected by the Orai pore geometry.PMID 23218667Read ↗

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

Gated regulation of CRAC channel ion selectivity by STIM1.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 ↗

Physiological CRAC channel activation and pore properties require STIM1 binding to all six Orai1 subunits.Semantic proximity Read ↗

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

Orai channel pore properties and gating by STIM: implications from the Orai crystal structure.Semantic proximity Read ↗

Native Store-operated Ca2+ Influx Requires the Channel Function of Orai1 and TRPC1.Semantic proximity Read ↗

Orai1 is an essential pore subunit of the CRAC channel.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 ↗

STIM1 activates CRAC channels through rotation of the pore helix to open a hydrophobic gate.Semantic proximity Read ↗

Sequential Steps of CRAC Channel Activation.Semantic proximity Read ↗

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