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(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
CaSR
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Poly-D-lysine hydrobromide (MW 30000-70000)
产品货号 : M35204
cas no: 27964-99-4
Poly-D-lysine hydrobromide (MW 30000-70000) 是一种人工合成的高分子基质,是神经细胞培养应用最广泛的基质之一。Poly-D-lysine hydrobromide (MW 30000-70000) 可从朊病毒感染的 SN56 神经母细胞瘤细胞中去除蛋白酶 K 抗性的 PrP,而不影响PrPC。 -
SB-423562
产品货号 : M26432
cas no: 351490-27-2
SB-423562 是一种钙敏感受体 (CaSR) 拮抗剂,可用于骨质疏松症的研究。 -
Gadolinium chloride
产品货号 : M23222
cas no: 10138-52-0
氯化钆是一种钙敏感受体 (CaSR) 激动剂。 -
Evocalcet
产品货号 : M22494
cas no: 870964-67-3
Evocalcet 对钙敏感受体 (CaSR) 具有激活作用。 -
Ronacaleret
产品货号 : M15865
cas no: 753449-67-1
一种有效的钙传感受体 (CaSR) 负变构调节剂,对于 hCaSR 的 IC50 为 146 nM。