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Target intelligence / Profile preview
Calcium-Sensing Receptor (CaSR)
- Target
- CaSR
- Molecular classification
- G protein-coupled receptor, GPCR, Class C GPCR
01
Overview
The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor (GPCR) that plays a central role in maintaining extracellular calcium ion (Ca2+) homeostasis. It senses small fluctuations in extracellular Ca2+ concentrations and modulates physiological responses accordingly. Dysfunction or mutations can lead to various calcium-related disorders.
- Other names
- Calcium receptorParathyroid calcium-sensing receptor 1PCaR1
02
Mechanism of action
Allosteric modulators affect the CaSR by stabilizing either the active or inactive receptor conformation, thus modulating its sensitivity to calcium. Agonist binding leads to compaction/dimerization via TM6 helix rearrangements.
03
Biological functions
Calcium homeostasis regulationParathyroid hormone (PTH) secretion regulationRenal tubular calcium reabsorption regulationCell proliferation modulationCell differentiation modulationSignal transduction
04
Disease associations
Familial benign hypocalciuric hypercalcemia (FBHH)Neonatal severe primary hyperparathyroidism (NSHPT)Adult primary hyperparathyroidismAutosomal-dominant hypocalcemia with hypercalciuriaHypocalcemiaHypercalcemiaSecondary hyperparathyroidism
05
Safety considerations
Hypocalcemia (with activating mutations or excessive calcimimetic use)Hypercalcemia (with inactivating mutations or auto-antibodies)Potential for off-target effects due to widespread tissue distribution
06
Interacting drugs
Calcimimetics (e.g., cinacalcet)
2 more in the full profile.
07
Biomarkers
Serum calcium levelsParathyroid hormone (PTH) levels
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