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CaSR

The calcium-sensing receptor (CaSR) is a G-protein coupled receptor (GPCR) that belongs to family (or class) C. Class C GPCRs are typified by large extracellular domains of around 450–600 amino acids. At the extreme N-terminus, just to the C-side of the signal peptide, is a large bilobed, nutrient-binding Venus Flytrap (VFT) domain of around 450–550 residues. The CaSR and other class C VFT domains are structurally related to bacterial nutrient-binding, periplasmic binding proteins,10 which act as sensors for the recruitment and activation of nutrient transporters. The CaSR activates various protein kinases including conventional isoforms of PKC, downstream of PI-PLC and Ca2+i mobilization, as well as mitogen-activated protein (MAP) kinases including ERK1/2, p38, and JNK and two key protein kinase regulators of cell fate, Akt and GSK-3.
The CaSR also couples to Rho kinase under the control of the monomeric G protein, Rho A35 and in the activation of the transcriptional modulator, Serum Response Factor (SRF). CaSR agonists and positive modulators induce pronounced stimulus-biased signaling with application to the understanding of diverse ligand-dependent physiological functions including L-amino acid-induced gut hormone release and Ca2+o-induced control of calcium homeostasis. These insights may also pave the way to the development

References

1.Conigrave AD,et al. Best Pract Res Clin Endocrinol Metab. 2013 Jun;27(3):315-31.

GPCR/G Protein

ACAT(2) Angiotensin Receptor(19) Antibacterial(231) Bombesin Receptor(7) Bradykinin Receptor(3) Calcium Channel(78) cAMP(3) Cannabinoid Receptor(42) CaSR(15) CGRP Receptor(9) Chemokine Receptor(104) Cholecystokinin Receptor(10) CRF Receptor(2) Dopamine Receptor(61) Endothelin Receptor(10) FFAR(5) Galanin Receptor(1) GHSR(7) Glucagon Receptor(11) GPCR19(3) GPR119(3) Hedgehog (Hh)(23) Histamine Receptor(77) Imidazoline Receptor(1) Leukotriene Receptor(6) LHR(1) LPA Receptor(3) Lysophospholipid Receptor(13) mAChR(23) MCHR(2) Melanocortin Receptor(7) Melatonin Receptor(5) mGluR(10) Motilin Receptor(2) Neurokinin Receptor(11) Neuropeptide Y Receptor(1) Neurotensin Receptor(1) Orexin Receptor(11) Other Targets(1) OXTR(2) P2Y Receptor(6) PAR(7) Platelet-activating Factor Receptor(2) Prostaglandin Receptor(28) PTH Receptor(1) S1P Receptor(7) SGLT(18) Somatostatin Receptor(5) Urotensin Receptor(1) Vasopressin Receptor(7)