Open AccessCalcium-sensing receptor (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database
Author(s) -
Daniel D. Bikle,
Hans BräunerOsborne,
Edward M. Brown,
Wenhan Chang,
Arthur D. Conigrave,
Fadil Hannan,
Katie Leach,
Daniela Riccardi,
Dolores Shoback,
Donald T. Ward,
Polina Yarova
Publication year - 2020
Publication title -
iuphar/bps guide to pharmacology cite
Language(s) - English
Resource type - Journals
ISSN - 2633-1020
DOI - 10.2218/gtopdb/f12/2020.5
Subject(s) - chemistry , divalent , calcium , extracellular , agonist , receptor , allosteric regulation , amino acid , biochemistry , ionic strength , peptide , organic chemistry , aqueous solution
The calcium-sensing receptor (CaS, provisional nomenclature as recommended by NC-IUPHAR [46] and subsequently updated [76]) 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 [77]). While divalent/trivalent cations, polyamines and polycations are CaS receptor agonists [14, 109], L-amino acids, glutamyl peptides, ionic strength and pH are allosteric modulators of agonist function [35, 46, 60, 107, 108]. Indeed, L-amino acids have been identified as "co-agonists", with both concomitant calcium and L-amino acid binding required for full receptor activation [147, 53]. The sensitivity of the CaS receptor to primary agonists is increased by elevated extracellular pH [17] or decreased extracellular ionic strength [108]. This receptor bears no sequence or structural relation to the plant calcium receptor, also called CaS.