Introduction of CASR
CASR is encoded by the CASR gene. CASR is a widely distributed G protein-coupled receptor. The human CASR gene is located on the long arm of chromosome 3 and consists of 1,078 amino acids and can be divided into three independent domains. The extracellular domain can form a dimer and then combine with polyvalent cations (Ca2+, Gd3+, and Mg2+), spermine, polyamines, multivalent antibiotics, and aromatic L-type amino acids to activate CASR and initiate downstream signal pathways that regulate cell function.
|Basic Information of CASR|
|Protein Name||Extracellular calcium-sensing receptor|
CAR, EIG8, FHH, FIH, GPRC2A, HHC, HHC1, HYPOC1, NSHPT, PCAR1,
calcium sensing receptor, hCasR, Calcium-sensing receptor+CaSR
|Organism||Homo sapiens (Human)|
Function of CASR Membrane Protein
CASR binds to extracellular Ca2+, CASR agonists, and allosteric modulators to activate itself, thereby directly activating G protein-coupled downstream signaling pathways. Its classical signal transduction pathway is mainly through the activation of CASR to hydrolyze phospholipase C (PLC) and phosphatidylinositol-4,5-bisphosphate, (PIP2), and release inositol-1, 4,5-triphosphate (IP3) and diacylglycerol (DAG). IP3 can bind to specific receptors on the surface of the endoplasmic reticulum and release a large amount of intracellular Ca2+. In addition, CASR plays an important role in maintaining cell membrane potential and homeostasis of metal ions such as Ca2+, Mg2+, and K+, regulating parathyroid hormone secretion, ion channel activation, and regulation of functional gene expression.
Fig.1 Structural basis for Mg2+/Ca2+ modulated CASR activities. (Chen, 2016)
Application of CASR Membrane Protein in Literature
The article showed that most patients with hereditary disease ADHH have a CASR gene mutation.
This article revealed that CASR can increase the vacuolar H + -ATPase activity of OKP cells, and the decrease of intracellular pH leads to an increase in intraluminal calcium ionization, which may enhance its reabsorption in the distal small tube segment and reduce the formation of calcium phosphate stones.
The article demonstrated that the expression of CASR in human bone marrow-derived MSCs, CASR plays an important role in regulating MSC fate and bone formation pathway selection.
This article indicated that R568 is a calcimimetic agent that activates CASR, which acts on intestinal epithelial cells and reverses cholera toxin-induced fluid secretion.
This article showed that CASR-promoting sensorimotor decisions are regulated by clathrin-mediated endocytosis by Gthi/o and Gαq/11 signaling.
CASR Preparation Options
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