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Extracellular calcium-sensing receptor (CaSR)
- Target
- CaSR
- Molecular classification
- G protein-coupled receptor, GPCR, Class C GPCR, Cell surface receptor
01
Overview
The extracellular calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor that senses changes in extracellular calcium ion (Ca2+) concentrations and maintains systemic calcium homeostasis. It is primarily expressed in the parathyroid gland and renal tubules, where it regulates parathyroid hormone (PTH) secretion and renal calcium reabsorption, respectively. Mutations or dysregulation of CaSR can cause various calcium-related disorders, and allosteric modulators are used clinically to treat conditions like secondary hyperparathyroidism.
02
Mechanism of action
Allosteric modulation (activation or inhibition) of CaSR activity.
03
Biological functions
Signal transductionCalcium homeostasisParathyroid hormone (PTH) secretion regulationRenal tubular reabsorption modulation
04
Disease associations
Familial benign hypocalciuric hypercalcemia (FBHH)Neonatal severe hyperparathyroidism (NSHPT)Adult primary hyperparathyroidismAutosomal-dominant hypocalcemia with hypercalciuriaHypocalcemia syndromesHypercalcemia syndromesSecondary hyperparathyroidism due to chronic kidney disease
05
Interacting drugs
Calcimimetics
1 more in the full profile.
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