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Calcium-sensing receptor C

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).

Overview

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The calcium-sensing receptor (CaS, provisional nomenclature as recommended by NC-IUPHAR [11] and subsequently updated [21]) responds to multiple endogenous ligands, including extracellular calcium and other divalent/trivalent cations, polyamines and polycationic peptides, L-amino acids (particularly L-Trp and L-Phe), glutathione and various peptide analogues, ionic strength and extracellular pH (reviewed in [22]). While divalent/trivalent cations, polyamines and polycations are CaS receptor agonists [3,33], L-amino acids, glutamyl peptides, ionic strength and pH are allosteric modulators of agonist function [8,11,16,31-32]. Indeed, L-amino acids have been identified as "co-agonists", with both concomitant calcium and L-amino acid binding required for full receptor activation [13,40]. The sensitivity of the CaS receptor to primary agonists is increased by elevated extracellular pH [4] or decreased extracellular ionic strength [32]. This receptor bears no sequence or structural relation to the plant calcium receptor, also called CaS.

Receptors

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Targets of relevance to immunopharmacology are highlighted in blue

CaS receptor C Show summary » More detailed page go icon to follow link

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Further reading

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: G protein-coupled receptors. Br J Pharmacol. 176 Issue S1: S21-S141.