Get Calcium-sensing Receptor essential facts below. View Videos or join the Calcium-sensing Receptor discussion. Add Calcium-sensing Receptor to your PopFlock.com topic list for future reference or share this resource on social media.
The release of PTH is inhibited in response to elevations in plasma calcium concentrations and activation of the calcium receptor. Increased calcium binding on the extracellular side gives a conformational change in the receptor, which, on the intracellular side, initiates the phospholipase C pathway, presumably through a Gq? type of G protein, which ultimately increases intracellular concentration of calcium, which inhibits vesicle fusion and exocytosis of parathyroid hormone. It also inhibits (not stimulates, as some sources state) the cAMP dependent pathway.
Calcilytic drugs, which block CaSR, produce increased bone density in animal studies and have been researched for the treatment of osteoporosis. Unfortunately clinical trial results in humans have proved disappointing, with sustained changes in bone density not observed despite the drug being well tolerated. More recent research has shown the CaSR receptor to be involved in numerous other conditions including Alzheimer's disease, asthma and some forms of cancer, and calcilytic drugs are being researched as potential treatments for these. Recently it has been shown that biomimetic bone like apatite inhibits formation of bone through endochondral ossification pathway via hyperstimulation of extracellular calcium sensing receptor.
^Giudice ML, Mihalik B, Dinnyés A, Kobolák J (July 2019). "The Nervous System Relevance of the Calcium Sensing Receptor in Health and Disease". Molecules. 24 (14): 2546. doi:10.3390/molecules24142546. PMID31336912.
^Vezzoli G, Soldati L, Gambaro G (April 2009). "Roles of calcium-sensing receptor (CaSR) in renal mineral ion transport". Current Pharmaceutical Biotechnology. 10 (3): 302-10. doi:10.2174/138920109787847475. PMID19355940.
^Torres PU (Jul 2006). "Cinacalcet HCl: a novel treatment for secondary hyperparathyroidism caused by chronic kidney disease". Journal of Renal Nutrition. 16 (3): 253-8. doi:10.1053/j.jrn.2006.04.010. PMID16825031.
^Nemeth EF, Shoback D (Jun 2013). "Calcimimetic and calcilytic drugs for treating bone and mineral-related disorders". Best Practice & Research. Clinical Endocrinology & Metabolism. 27 (3): 373-84. doi:10.1016/j.beem.2013.02.008. PMID23856266.
^John MR, Harfst E, Loeffler J, Belleli R, Mason J, Bruin GJ, Seuwen K, Klickstein LB, Mindeholm L, Widler L, Kneissel M (Jul 2014). "AXT914 a novel, orally-active parathyroid hormone-releasing drug in two early studies of healthy volunteers and postmenopausal women". Bone. 64: 204-10. doi:10.1016/j.bone.2014.04.015. PMID24769332.
Aida K, Koishi S, Inoue M, Nakazato M, Tawata M, Onaya T (Sep 1995). "Familial hypocalciuric hypercalcemia associated with mutation in the human Ca(2+)-sensing receptor gene". The Journal of Clinical Endocrinology and Metabolism. 80 (9): 2594-8. doi:10.1210/jc.80.9.2594. PMID7673400.
Aida K, Koishi S, Tawata M, Onaya T (Sep 1995). "Molecular cloning of a putative Ca(2+)-sensing receptor cDNA from human kidney". Biochemical and Biophysical Research Communications. 214 (2): 524-9. doi:10.1006/bbrc.1995.2318. PMID7677761.
Pollak MR, Brown EM, Estep HL, McLaine PN, Kifor O, Park J, Hebert SC, Seidman CE, Seidman JG (Nov 1994). "Autosomal dominant hypocalcaemia caused by a Ca(2+)-sensing receptor gene mutation". Nature Genetics. 8 (3): 303-7. doi:10.1038/ng1194-303. PMID7874174. S2CID22941518.
Pollak MR, Brown EM, Chou YH, Hebert SC, Marx SJ, Steinmann B, Levi T, Seidman CE, Seidman JG (Dec 1993). "Mutations in the human Ca(2+)-sensing receptor gene cause familial hypocalciuric hypercalcemia and neonatal severe hyperparathyroidism". Cell. 75 (7): 1297-303. doi:10.1016/0092-8674(93)90617-Y. PMID7916660. S2CID40886966.
Janicic N, Soliman E, Pausova Z, Seldin MF, Rivière M, Szpirer J, Szpirer C, Hendy GN (Nov 1995). "Mapping of the calcium-sensing receptor gene (CASR) to human chromosome 3q13.3-21 by fluorescence in situ hybridization, and localization to rat chromosome 11 and mouse chromosome 16". Mammalian Genome. 6 (11): 798-801. doi:10.1007/BF00539007. PMID8597637. S2CID19835161.
Chattopadhyay N, Ye C, Singh DP, Kifor O, Vassilev PM, Shinohara T, Chylack LT, Brown EM (Apr 1997). "Expression of extracellular calcium-sensing receptor by human lens epithelial cells". Biochemical and Biophysical Research Communications. 233 (3): 801-5. doi:10.1006/bbrc.1997.6553. PMID9168937.
Cole DE, Janicic N, Salisbury SR, Hendy GN (Aug 1997). "Neonatal severe hyperparathyroidism, secondary hyperparathyroidism, and familial hypocalciuric hypercalcemia: multiple different phenotypes associated with an inactivating Alu insertion mutation of the calcium-sensing receptor gene". American Journal of Medical Genetics. 71 (2): 202-10. doi:10.1002/(SICI)1096-8628(19970808)71:2<202::AID-AJMG16>3.0.CO;2-I. PMID9217223.