Recombinant Human CaSR protein (GST tag N-Terminus)

Specifications

Form

Liquid

General info

Function

G-protein-coupled receptor that senses changes in the extracellular concentration of calcium ions and plays a key role in maintaining calcium homeostasis (PubMed : 17555508, PubMed : 19789209, PubMed : 21566075, PubMed : 22114145, PubMed : 22789683, PubMed : 23966241, PubMed : 25104082, PubMed : 25292184, PubMed : 25766501, PubMed : 26386835, PubMed : 32817431, PubMed : 33603117, PubMed : 34194040, PubMed : 34467854, PubMed : 7759551, PubMed : 8636323, PubMed : 8702647, PubMed : 8878438). Senses fluctuations in the circulating calcium concentration : activated by elevated circulating calcium, leading to decreased parathyroid hormone (PTH) secretion in parathyroid glands (By similarity). In kidneys, acts as a key regulator of renal tubular calcium resorption (By similarity). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G-proteins) and modulates the activity of downstream effectors (PubMed : 38632411). CASR is coupled with different G(q)/G(11), G(i)/G(o)- or G(s)-classes of G-proteins depending on the context (PubMed : 38632411). In the parathyroid and kidney, CASR signals through G(q)/G(11) and G(i)/G(o) G-proteins : G(q)/G(11) coupling activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers, while G(i)/G(o) coupling mediates inhibition of adenylate cyclase activity (PubMed : 38632411, PubMed : 7759551). The G-protein-coupled receptor activity is activated by a co-agonist mechanism : aromatic amino acids, such as Trp or Phe, act concertedly with divalent cations, such as calcium or magnesium, to achieve full receptor activation (PubMed : 27386547, PubMed : 27434672, PubMed : 32817431, PubMed : 33603117, PubMed : 34194040). Acts as an activator of the NLRP3 inflammasome via G(i)/G(o)-mediated signaling : down-regulation of cyclic AMP (cAMP) relieving NLRP3 inhibition by cAMP (PubMed : 32843625). Acts as a regulator of proton-sensing receptor GPR68 in a seesaw manner : CASR-mediated signaling inhibits GPR68 signaling in response to extracellular calcium, while GPR68 inhibits CASR in presence of extracellular protons (By similarity).

Sequence similarities

Belongs to the G-protein coupled receptor 3 family.

Post-translational modifications

Phosphorylation at Thr-888 by PKC impairs coupling with G(q)/G(11) G-proteins, while it does not affect G(i)/G(o)-coupling (PubMed:17376781, PubMed:38326620, PubMed:9694886). Phosphorylation at Ser-892 by PKC and Ser-899 by PKA promote plasma membrane localization (PubMed:20798521).. Ubiquitinated by RNF19A; which induces proteasomal degradation.. N-glycosylated.