Sensing Extracellular Calcium – An Insight into the Structure and Function of the Calcium-Sensing Receptor (CaSR)

Sergei Chavez-Abiega, Iris Mos, Patricia P. Centeno, Taha Elajnaf, Wolfgang Schlattl, Donald T. Ward, Joachim Goedhart, Enikö Kallay

Research output: Chapter in Book / Report / Conference proceedingChapterAcademicpeer-review

Abstract

The calcium-sensing receptor (CaSR) is a G protein-coupled receptor that plays a key role in calcium homeostasis, by sensing free calcium levels in blood and regulating parathyroid hormone secretion in response. The CaSR is highly expressed in parathyroid gland and kidney where its role is well characterised, but also in other tissues where its function remains to be determined. The CaSR can be activated by a variety of endogenous ligands, as well as by synthetic modulators such as Cinacalcet, used in the clinic to treat secondary hyperparathyroidism in patients with chronic kidney disease. The CaSR couples to multiple G proteins, in a tissue-specific manner, activating several signalling pathways and thus regulating diverse intracellular events. The multifaceted nature of this receptor makes it a valuable therapeutic target for calciotropic and non-calciotropic diseases. It is therefore essential to understand the complexity behind the pharmacology, trafficking, and signalling characteristics of this receptor. This review provides an overview of the latest knowledge about the CaSR and discusses future hot topics in this field.

Original languageEnglish
Title of host publicationCalcium Signaling
EditorsShahidul Islam
Place of PublicationCham
PublisherSpringer Nature Switzerland AG
Chapter41
Pages1031-1063
Number of pages33
Edition2nd
ISBN (Electronic)9783030124571
ISBN (Print)9783030124564
DOIs
Publication statusPublished - 2020

Publication series

NameAdvances in Experimental Medicine and Biology
Volume1131
ISSN (Print)0065-2598
ISSN (Electronic)2214-8019

Fingerprint

Calcium-Sensing Receptors
Calcium
Tissue
Secondary Hyperparathyroidism
Parathyroid Glands
G-Protein-Coupled Receptors
Parathyroid Hormone
Chronic Renal Insufficiency
GTP-Binding Proteins
Modulators
Homeostasis
Blood
Pharmacology
Ligands
Kidney

Keywords

  • Allosteric modulators
  • Biased signalling
  • Calcilytics
  • Calcimimetics
  • Cellular trafficking
  • Extracellular calcium
  • G protein-coupled receptor
  • G proteins
  • Orthosteric ligands
  • Parathyroid hormone

Cite this

Chavez-Abiega, S., Mos, I., Centeno, P. P., Elajnaf, T., Schlattl, W., Ward, D. T., ... Kallay, E. (2020). Sensing Extracellular Calcium – An Insight into the Structure and Function of the Calcium-Sensing Receptor (CaSR). In S. Islam (Ed.), Calcium Signaling (2nd ed., pp. 1031-1063). (Advances in Experimental Medicine and Biology; Vol. 1131). Cham: Springer Nature Switzerland AG. https://doi.org/10.1007/978-3-030-12457-1_41
Chavez-Abiega, Sergei ; Mos, Iris ; Centeno, Patricia P. ; Elajnaf, Taha ; Schlattl, Wolfgang ; Ward, Donald T. ; Goedhart, Joachim ; Kallay, Enikö. / Sensing Extracellular Calcium – An Insight into the Structure and Function of the Calcium-Sensing Receptor (CaSR). Calcium Signaling. editor / Shahidul Islam. 2nd. ed. Cham : Springer Nature Switzerland AG, 2020. pp. 1031-1063 (Advances in Experimental Medicine and Biology).
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Chavez-Abiega, S, Mos, I, Centeno, PP, Elajnaf, T, Schlattl, W, Ward, DT, Goedhart, J & Kallay, E 2020, Sensing Extracellular Calcium – An Insight into the Structure and Function of the Calcium-Sensing Receptor (CaSR). in S Islam (ed.), Calcium Signaling. 2nd edn, Advances in Experimental Medicine and Biology, vol. 1131, Springer Nature Switzerland AG, Cham, pp. 1031-1063. https://doi.org/10.1007/978-3-030-12457-1_41

Sensing Extracellular Calcium – An Insight into the Structure and Function of the Calcium-Sensing Receptor (CaSR). / Chavez-Abiega, Sergei; Mos, Iris; Centeno, Patricia P.; Elajnaf, Taha; Schlattl, Wolfgang; Ward, Donald T.; Goedhart, Joachim; Kallay, Enikö.

Calcium Signaling. ed. / Shahidul Islam. 2nd. ed. Cham : Springer Nature Switzerland AG, 2020. p. 1031-1063 (Advances in Experimental Medicine and Biology; Vol. 1131).

Research output: Chapter in Book / Report / Conference proceedingChapterAcademicpeer-review

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Chavez-Abiega S, Mos I, Centeno PP, Elajnaf T, Schlattl W, Ward DT et al. Sensing Extracellular Calcium – An Insight into the Structure and Function of the Calcium-Sensing Receptor (CaSR). In Islam S, editor, Calcium Signaling. 2nd ed. Cham: Springer Nature Switzerland AG. 2020. p. 1031-1063. (Advances in Experimental Medicine and Biology). https://doi.org/10.1007/978-3-030-12457-1_41