New insights into the role of calcium-sensing receptor activation

Abstract

The discovery of the calcium-sensing receptor (CaSR) prompted the identification of substances that affect its function. Cinacalcet, for example, is a drug that allosterically modifies the receptor so as to increase its sensitivity to circulating calcium (thus the name "calcimimetic") and in this way decreases parathyroid hormone secretion. Clinical use of cinacalcet is already approved for the treatment of primary and secondary hyperparathyroidism, but research is ongoing to identify further potential actions of this drug. The effects and functions of the CaSR have been evaluated in different systems and tissues, beyond parathyroid glands, such arterial walls. A complete understanding of the properties of calcimimetics are of obvious clinical interest, since therapeutic indications may be affected accordingly.