Orai2 | Orai channels | IUPHAR/BPS Guide to PHARMACOLOGY

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target has curated data in GtoImmuPdb

Target id: 2965

Nomenclature: Orai2

Family: Orai channels

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 254 7q22.1 ORAI2 ORAI calcium release-activated calcium modulator 2
Mouse 4 250 5 G2 Orai2 ORAI calcium release-activated calcium modulator 2
Rat 4 - 12q12 Orai2 ORAI calcium release-activated calcium modulator 2
Previous and Unofficial Names
CAP-binding protein complex interacting protein 2 | CBCIP2 | TMEM142B
Database Links
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein

Download all structure-activity data for this target as a CSV file

Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
CM4620 Hs Inhibition 6.1 pIC50 - no 4
pIC50 6.1 (IC50 8.95x10-7 M) [4]
Not voltage dependent
Description: In vitro inhibition of calcium entry mediated by Orai2/STIM1 CRAC channels.
GSK-7975A Hs Inhibition 5.8 pIC50 - no 4
pIC50 5.8 (IC50 1.453x10-6 M) [4]
Not voltage dependent
Description: In vitro inhibition of calcium entry mediated by Orai2/STIM1 CRAC channels.
Immunopharmacology Comments
The ORAI1 and ORAI2 proteins form heteromeric complexes that constitute the pore of Ca2+ release-activated Ca2+ (CRAC) channels. CRAC channels mediate store-operated Ca2+ entry (SOCE), a function that is essential for proper T cell function. Evidence indicates that ORAI2 fine-tunes SOCE to modulate the immune response [3]. Mice with double Orai1/Orai2 knockout have severely impaired T cell function and T cell-dependent antiviral immune responses. Conversely, these mice are protected from T cell-mediated autoimmunity and alloimmunity.
Cell Type Associations
Immuno Cell Type:  T cells
Comment:  Orai2 (along with Orai1) is involved in T cell -mediated immune responses (demonstrated in mice in vivo).
References:  2
Physiological Consequences of Altering Gene Expression
Deletion of Orai2 increases store-operated Ca2+ entry (SOCE) in mouse T cells.
Species:  Mouse
Tissue:  T cells
References:  3
Deletion of Orai2 in murine peritoneal mast cells augments endogenous CRAC currents and degranulation.
Species:  Mouse
Tissue:  Peritoneal mast cells
Technique:  Targeted inactivation of the Orai2 gene.
References:  1


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1. Tsvilovskyy V, Solís-López A, Schumacher D, Medert R, Roers A, Kriebs U, Freichel M. (2018) Deletion of Orai2 augments endogenous CRAC currents and degranulation in mast cells leading to enhanced anaphylaxis. Cell Calcium, 71: 24-33. [PMID:29604961]

2. Vaeth M, Feske S. (2018) Ion channelopathies of the immune system. Curr. Opin. Immunol., 52: 39-50. [PMID:29635109]

3. Vaeth M, Yang J, Yamashita M, Zee I, Eckstein M, Knosp C, Kaufmann U, Karoly Jani P, Lacruz RS, Flockerzi V et al.. (2017) ORAI2 modulates store-operated calcium entry and T cell-mediated immunity. Nat Commun, 8: 14714. [PMID:28294127]

4. Velicelebi G, Stauderman K, Dunn M, Roos J. (2016) Pancreatitis treatment. Patent number: WO2016138472A1. Assignee: Calcimedica, Inc.. Priority date: 27/02/2015. Publication date: 01/09/2016.

How to cite this page

Orai channels: Orai2. Last modified on 17/10/2018. Accessed on 21/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2965.