Calcium-Sensing GPCR Family Subtypes and Products

What Are Calcium-Sensing Receptors?

The calcium-sensing receptor (CaSR) belongs to the family C G-protein coupled receptors (GPCRs). CaSR is expressed in the parathyroid gland, where it regulates the release of parathyroid hormone, maintaining calcium homeostasis. CaSR antagonists have undergone clinical trials to test their validity as an osteoporosis treatment, with suboptimal results. Research is currently being done on the potential of CaSR antagonists as treatments for asthma and Alzheimer’s. Allosteric modifiers to CaSR, such as the drugs cinacalcet and etelcalcetide, are used to treat hyperthyroidism by decreasing the release of parathyroid hormone.

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Calcium-Sensing Receptor Information

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CaSR

CASR is a calcium-sensing receptor and plays an important role in regulating PTH secretion. It is expressed in many different tissues, such as parathyroid cells, pituitary cells, kidney, fibroblasts, keratinocytes and human colon epithelial cells. CASR is a potential therapeutic target for the treatment of many diseases, including hyperparathyroidism and osteoporosis. Mutations in the CASR gene can result in gain or loss of receptor function. Familial Hypocalciuric Hypercalcemia (FHH) and Neonatal Severe Primary Hyperparathyroidism (NSHPT) have been associated with loss of CASR function, while Autosomal Dominant Hypocalcemia (ADH) and Bartter syndrome type V have been associated with gain of CASR function.

Calcium-Sensing Cell Lines

Receptor Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Calcium-Sensing	CaSR	human	HEK293T	C1233	DC1233	MC1233
Calcium-Sensing	CaSR	rat	HEK293T	Hr1233	DHr1233	MHr1233