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Protein A004000
Author-entered Data
V1.0, Peer Reviewed
Published 5 Jun 2008
Automated Data
Not Reviewed
As At Publication
Automated Data
Not Reviewed
Latest from 6 Jun 2014

UCSD Nature Molecule Pages
Published online: 5 Jun 2008 | doi:10.1038/mp.a004000.01

Calcium-sensing receptor

Basis Sequence: Mouse

Noriko Makita1, Taroh Iiri1

1Endocrinology and Nephrology, The University of Tokyo, 113-8655, JP.

Correspondence should be addressed to Taroh Iiri: tiiri-tky@umin.ac.jp


The calcium-sensing receptor (CaSR) belongs to the G-protein-coupled receptor (GPCR) family C and has a key role in calcium homeostasis by sensing changes in the concentration of its agonist, the extracellular calcium ion (Ca2+o). CaSR is mainly expressed in parathyroid and renal tubular epithelial cells, but is also found in multiple different cell types in many organs. In parathyroid cells, CaSR regulates three key elements of parathyroid function: the synthesis and secretion of parathyroid hormone (PTH), and the proliferation of parathyroid cells. When the concentration of Ca2+o increases, the secretion of PTH immediately decreases via a negative feedback loop, thus enabling the precise control of the Ca2+o levels. The main functions of CaSR at the molecular level include the activation of Gq/11 and Gi/o, that results in the activation of phospholipase C, the inhibition of adenylyl cyclase, and the modulation of the mitogen-activated protein kinases (MAPKs). However, it is not yet known which signaling systems convey the PTH and growth effects. Mutations in the CaSR gene and the actions of autoantibodies against the receptor itself underlie the pathophysiology of both familial and acquired mineral metabolism disorders. Therefore, positive and negative allosteric modulators of CaSR have the potential to treat disorders of calcium homeostasis and some such compounds have been developed as drugs for this purpose.

Alternative names for this molecule: Calcium receptor; Calcium-sensing receptor; CaR; CaSR; Casr; cation sensing receptor; extracellular calcium-sensing receptor; Extracellular calcium-sensing receptor precursor; G protein coupled receptor, family C, group 2, member A; G protein-coupled receptor, family C, group 2, member A; Gprc2a; Parathyroid Cell calcium-sensing receptor

Transition Network Graph This molecule exists in 41 states, has 60 transitions between these states and has 19 receptor functions.

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