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Research ArticleMinireview

Agonists and allosteric modulators of the Calcium Sensing Receptor and their therapeutic applications

Zuzana Saidak, Michel Brazier, Said Kamel and Romuald Mentaverri
Molecular Pharmacology September 24, 2009, mol.109.058784; DOI: https://doi.org/10.1124/mol.109.058784
Zuzana Saidak
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Michel Brazier
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Said Kamel
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Romuald Mentaverri
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Abstract

The Calcium sensing Receptor (CaR) belongs to the G protein-coupled receptor superfamily, with a characteristic structure consisting of seven transmembrane helices, an intracellular C terminal and an extracellular N terminal domain. The primary physiological function of the CaR is the maintenance of constant blood Ca2+ levels, due to its ability to sense very small changes in extracellular Ca2+ (Ca2+o) concentrations. Nevertheless, in addition to being expressed in tissues involved in Ca2+o homeostasis, the CaR is also expressed in tissues not involved in mineral homeostasis, suggestive of additional physiological functions. Numerous agonists and modulators of the CaR are now known in addition to Ca2+o, including various divalent and trivalent cations, aromatic L-amino acids, polyamines, and aminoglycoside antibiotics. The signaling of the CaR is also regulated by extracellular pH and ionic strength. The activated CaR couples mainly to the phospholipase Cβ and ERK1/2 signaling pathways, and it decreases intracellular cAMP levels, leading to various physiological effects. The recent identification of synthetic allosteric modulators of the CaR has opened up a new field of research possibilities. Calcimimetics and calcilytics, which increase and decrease agonist signaling via the CaR, respectively, may facilitate the manipulation of the CaR, and thus aid in further investigations of its precise signaling. These allosteric modulators, as well as strontium, have been demonstrated to have therapeutic potential for the treatment of disorders involving the CaR. This review discusses the various agonists and modulators of the CaR, differences in their binding and signaling, and their roles as therapeutics in various diseases.

  • Gi family
  • Gq/11 family
  • Calcium (G Protein Coupled Signals)

Footnotes

    • Received June 23, 2009.
    • Revision received September 24, 2009.
    • Accepted September 24, 2009.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 103 (2)
Molecular Pharmacology
Vol. 103, Issue 2
1 Feb 2023
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Research ArticleMinireview

Agonists and allosteric modulators of the Calcium Sensing Receptor and their therapeutic applications

Zuzana Saidak, Michel Brazier, Said Kamel and Romuald Mentaverri
Molecular Pharmacology September 24, 2009, mol.109.058784; DOI: https://doi.org/10.1124/mol.109.058784

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Research ArticleMinireview

Agonists and allosteric modulators of the Calcium Sensing Receptor and their therapeutic applications

Zuzana Saidak, Michel Brazier, Said Kamel and Romuald Mentaverri
Molecular Pharmacology September 24, 2009, mol.109.058784; DOI: https://doi.org/10.1124/mol.109.058784
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