Calcium-sensing receptor (CaSR), a member of family C of the G protein-coupled receptors, is expressed most abundantly in the parathyroid glands and kidney. It plays key role in these two organs because it senses changes in extracellular calcium and regulates PTH secretion and calcium reabsorption to suit the extracellular calcium concentration.

An Overview of CaSR

Calcium-sensing receptor (CaSR) is a member of GPCRs superfamily. Since Brown et al first cloned it from bovine parathyroid cells in 1993, its role in organism has received increasing attention. It has been shown that CaSR can maintain and regulate the balance of intracellular Ca2+ and other mineral ions. It also participates in cell secretion, proliferation, differentiation, chemotaxis, apoptosis, gene expression, maintenance of membrane potential, and ion channel switch, the regulation of senescence and other processes. CaSR is widely distributed in tissues that regulate intracellular calcium homeostasis, such as thyroid gland, parathyroid gland, kidney, gastrointestinal tract, bone tissue, and other organs such as vascular smooth muscle, nervous system, pancreas, bone marrow, etc. It’s also expressed in pituitary and mammary glands. In recent years, the expression of CaSR has been found in rat mononuclear/macrophage cell lines, peripheral blood progenitor cells, platelets and human T lymphocytes. The human CaSR gene is located on the arm of chromosome 3 and consists of 1078 amino acids, including three domains.

Inhibition of CaSR

NPS-2143 (SB 262470) is a selective calcium ion-sensitive receptor antagonist with IC (50) of 43 nm and 41 nm, respectively, which can inhibit intracellular Ca2+ concentration and parathyroid hormone secretion.

CaSR and diseases

The effect of CaSR on cardiac myocytes in type I diabetic cardiomyopathy is opposite to that in rat type I diabetic cardiomyopathy. It increases the degree of myocardial cell damage in type I-diabetic cardiomyopathy. The expression of CaSR is significantly decreased in breast cancer cells, and CaSR can be used as an independent marker to predict the prognosis of breast cancer. In metastatic bone tumors of renal cell carcinoma (RCC), the role of extracellular CaSR in promoting metastasis and proliferation of tumor cells is achieved through the high expression of CaSR and its downstream pathway. In the forefront of bone metastasis, the expression of CaSR in adenocarcinoma cell line is significantly higher than that in prostate cancer cell line without bone metastasis.

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