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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
The inositol 1,4,5-trisphosphate receptors (IP3R) are ligand-gated Ca2+-release channels on intracellular Ca2+ store sites (such as the endoplasmic reticulum). They are responsible for the mobilization of intracellular Ca2+ stores and play an important role in intracellular Ca2+ signalling in a wide variety of cell types. Three different gene products (types I–III) have been isolated, which assemble as large tetrameric structures. IP3Rs are closely associated with certain proteins: calmodulin (CALM2, CALM3, CALM1, P62158) and FKBP (and calcineurin via FKBP). They are phosphorylated by PKA, PKC, PKG and CaMKII.
* Key recommended reading is highlighted with an asterisk
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* Barker CJ, Berggren PO. (2013) New horizons in cellular regulation by inositol polyphosphates: insights from the pancreatic β-cell. Pharmacol. Rev., 65 (2): 641-69. [PMID:23429059]
Berridge MJ, Lipp P, Bootman MD. (2000) The versatility and universality of calcium signalling. Nat. Rev. Mol. Cell Biol., 1 (1): 11-21. [PMID:11413485]
Bolton TB. (2006) Calcium events in smooth muscles and their interstitial cells; physiological roles of sparks. J. Physiol. (Lond.), 570 (Pt 1): 5-11. [PMID:16195319]
Bootman MD, Berridge MJ, Roderick HL. (2002) Calcium signalling: more messengers, more channels, more complexity. Curr. Biol., 12 (16): R563-5. [PMID:12194839]
Bosanac I, Michikawa T, Mikoshiba K, Ikura M. (2004) Structural insights into the regulatory mechanism of IP3 receptor. Biochim. Biophys. Acta, 1742 (1-3): 89-102. [PMID:15590059]
Bultynck G, Sienaert I, Parys JB, Callewaert G, De Smedt H, Boens N, Dehaen W, Missiaen L. (2003) Pharmacology of inositol trisphosphate receptors. Pflugers Arch., 445 (6): 629-42. [PMID:12632182]
Choe CU, Ehrlich BE. (2006) The inositol 1,4,5-trisphosphate receptor (IP3R) and its regulators: sometimes good and sometimes bad teamwork. Sci. STKE, 2006 (363): re15. [PMID:17132820]
* Decrock E, De Bock M, Wang N, Gadicherla AK, Bol M, Delvaeye T, Vandenabeele P, Vinken M, Bultynck G, Krysko DV et al.. (2013) IP3, a small molecule with a powerful message. Biochim. Biophys. Acta, 1833 (7): 1772-86. [PMID:23291251]
* Foskett JK. (2010) Inositol trisphosphate receptor Ca2+ release channels in neurological diseases. Pflugers Arch., 460 (2): 481-94. [PMID:20383523]
Foskett JK, White C, Cheung KH, Mak DO. (2007) Inositol trisphosphate receptor Ca2+ release channels. Physiol. Rev., 87 (2): 593-658. [PMID:17429043]
* Kiviluoto S, Vervliet T, Ivanova H, Decuypere JP, De Smedt H, Missiaen L, Bultynck G, Parys JB. (2013) Regulation of inositol 1,4,5-trisphosphate receptors during endoplasmic reticulum stress. Biochim. Biophys. Acta, 1833 (7): 1612-24. [PMID:23380704]
Mikoshiba K. (2007) IP3 receptor/Ca2+ channel: from discovery to new signaling concepts. J. Neurochem., 102 (5): 1426-46. [PMID:17697045]
Mikoshiba K. (2007) The IP3 receptor/Ca2+ channel and its cellular function. Biochem. Soc. Symp., (74): 9-22. [PMID:17233576]
Nahorski SR. (2006) Pharmacology of intracellular signalling pathways. Br. J. Pharmacol., 147 Suppl 1: S38-45. [PMID:16402119]
Patel S, Joseph SK, Thomas AP. (1999) Molecular properties of inositol 1,4,5-trisphosphate receptors. Cell Calcium, 25 (3): 247-64. [PMID:10378086]
Patterson RL, Boehning D, Snyder SH. (2004) Inositol 1,4,5-trisphosphate receptors as signal integrators. Annu. Rev. Biochem., 73: 437-65. [PMID:15189149]
* Rossi AM, Tovey SC, Rahman T, Prole DL, Taylor CW. (2012) Analysis of IP3 receptors in and out of cells. Biochim. Biophys. Acta, 1820 (8): 1214-27. [PMID:22033379]
Taylor CW, Tovey SC. (2010) IP(3) receptors: toward understanding their activation. Cold Spring Harb Perspect Biol, 2 (12): a004010. [PMID:20980441]
Taylor CW, Traynor D. (1995) Calcium and inositol trisphosphate receptors. J. Membr. Biol., 145 (2): 109-18. [PMID:7563013]
Verkhratsky A. (2005) Physiology and pathophysiology of the calcium store in the endoplasmic reticulum of neurons. Physiol. Rev., 85 (1): 201-79. [PMID:15618481]
Vermassen E, Parys JB, Mauger JP. (2004) Subcellular distribution of the inositol 1,4,5-trisphosphate receptors: functional relevance and molecular determinants. Biol. Cell, 96 (1): 3-17. [PMID:15093123]
Database page citation:
IP3 receptor. Accessed on 27/08/2016. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=123.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Peters JA, Kelly E, Marrion N, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Ligand-gated ion channels. Br J Pharmacol. 172: 5870-5903.