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.
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(3)
Angiotensin Receptor(27)
Antibacterial(471)
Bombesin Receptor(11)
Bradykinin Receptor(18)
Calcium Channel(137)
cAMP(9)
Cannabinoid Receptor(69)
CaSR(17)
CGRP Receptor(14)
Chemokine Receptor(104)
Cholecystokinin Receptor(17)
CRF Receptor(13)
Dopamine Receptor(145)
Endothelin Receptor(20)
FFAR(5)
Galanin Receptor(1)
GHSR(16)
Glucagon Receptor(36)
GPCR19(7)
GPR119(3)
Hedgehog (Hh)(27)
Histamine Receptor(110)
Imidazoline Receptor(1)
Leukotriene Receptor(9)
LHR(1)
LPA Receptor(12)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(6)
Melanocortin Receptor(22)
Melatonin Receptor(5)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(34)
Neuropeptide Y Receptor(36)
Neurotensin Receptor(8)
Orexin Receptor(14)
Other Targets(3)
OXTR(2)
P2Y Receptor(8)
PAR(24)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(60)
PTH Receptor(1)
S1P Receptor(22)
SGLT(22)
Somatostatin Receptor(11)
Urotensin Receptor(4)
Vasopressin Receptor(16)
CaSR
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SB-423562
catalog no : M26432
cas no: 351490-27-2
SB-423562 is a calcium-sensing receptor (CaSR) antagonist and can be used in studies about osteoporosis. -
Gadolinium chloride
catalog no : M23222
cas no: 10138-52-0
Gadolinium chloride is a calcium-sensing receptor (CaSR) agonist. -
Evocalcet
catalog no : M22494
cas no: 870964-67-3
Evocalcet has an activating effect on the calcium-sensing receptor (CaSR). -
Ronacaleret
catalog no : M15865
cas no: 753449-67-1
A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR. -
Calindol hydrochloride
catalog no : M15792
cas no: 729610-18-8
Calindol hydrochloride is a calcimimetic acting agent and positive allosteric modulator (agonist) of CaSR with EC50 of 0.31 uM.