Allosteric modulation of the calcium-sensing receptor

AA Jensen, H Brauner-Osborne - Current neuropharmacology, 2007 - ingentaconnect.com
The calcium (Ca2+)-sensing receptor (CaR) belongs to family C of the G-protein coupled
receptors (GPCRs). The receptor is activated by physiological levels of Ca2+ (and Mg2+) …

Agonists and allosteric modulators of the calcium-sensing receptor and their therapeutic applications

Z Saidak, M Brazier, S Kamel, R Mentaverri - Molecular pharmacology, 2009 - ASPET
The calcium-sensing receptor (CaR) belongs to the G protein-coupled receptor superfamily,
with a characteristic structure consisting of seven transmembrane helices, an intracellular C …

Allosteric modulators of the extracellular calcium receptor

EF Nemeth - Drug Discovery Today: Technologies, 2013 - Elsevier
The extracellular calcium receptor (CaR) is a Family CG protein-coupled receptor that
controls systemic Ca2+ homeostasis, largely by regulating the secretion of parathyroid …

Discovery and development of calcimimetic and calcilytic compounds

EF Nemeth, BC Van Wagenen, MF Balandrin - Progress in Medicinal …, 2018 - Elsevier
The extracellular calcium receptor (CaR) is a G protein-coupled receptor (GPCR) and the
pivotal molecule regulating systemic Ca 2+ homeostasis. The CaR was a challenging target …

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics

AE Cook, SN Mistry, KJ Gregory… - British journal of …, 2015 - Wiley Online Library
Background and Purpose Clinical use of cinacalcet in hyperparathyroidism is complicated
by its tendency to induce hypocalcaemia, arising partly from activation of calcium‐sensing …

Recent updates on the calcium-sensing receptor as a drug target

R Trivedi, A Mithal… - Current medicinal …, 2008 - ingentaconnect.com
Parathyroid hormone (PTH) secreted from parathyroid cells is a key regulator of circulating
levels of calcium ion, which is maintained within a narrow physiological range mainly by the …

New concepts in calcium‐sensing receptor pharmacology and signalling

DT Ward, D Riccardi - British journal of pharmacology, 2012 - Wiley Online Library
The calcium‐sensing receptor (CaR) is the key controller of extracellular calcium (Ca2+ o)
homeostasis via its regulation of parathyroid hormone (PTH) secretion and renal Ca2+ …

Calcium sensing receptor activators: calcimimetics

PE Harrington, C Fotsch - Current medicinal chemistry, 2007 - ingentaconnect.com
The calcium sensing receptor (CaR) is a G protein-coupled receptor (GPCR) that plays a
fundamental role in serum calcium homeostasis. The CaR is expressed on the chief cells of …

[HTML][HTML] Pharmacology of the calcium sensing receptor

M Filopanti, S Corbetta, AM Barbieri… - Clinical Cases in …, 2013 - ncbi.nlm.nih.gov
Calcium sensing receptor (CASR) is a G-protein couple receptor which plays a key role in
calcium homeostasis in vertebrates. Its extracellular domain is sensitive to divalent cations …

Novel strategies in drug discovery of the calcium-sensing receptor based on biased signaling

A Rojas Bie Thomsen, S Smajilovic… - Current drug …, 2012 - ingentaconnect.com
A hallmark of chronic kidney disease is hyperphosphatemia due to renal phosphate
retention. Prolonged parathyroid gland exposure to hyperphosphatemia leads to secondary …