The calcimimetic cinacalcet normalizes serum calcium in subjects with primary hyperparathyroidism

DM Shoback, JP Bilezikian, SA Turner… - The Journal of …, 2003 - academic.oup.com
Calcimimetics increase the sensitivity of the calcium-sensing receptor (CaR) to circulating
serum calcium, reducing the secretion of PTH and the serum calcium concentration. We …

[HTML][HTML] Homology modeling of the transmembrane domain of the human calcium sensing receptor and localization of an allosteric binding site

SU Miedlich, L Gama, K Seuwen, RM Wolf… - Journal of Biological …, 2004 - ASBMB
A homology model for the human calcium sensing receptor (hCaR) transmembrane domain
utilizing bovine rhodopsin (bRho) structural information was derived and tested by docking …

Calcimimetic and calcilytic therapies for inherited disorders of the calcium‐sensing receptor signalling pathway

FM Hannan, MK Olesen… - British Journal of …, 2018 - Wiley Online Library
The calcium‐sensing receptor (CaS receptor) plays a pivotal role in extracellular calcium
homeostasis, and germline loss‐of‐function and gain‐of‐function mutations cause familial …

Allosteric modulators of class-C G-protein-coupled receptors open new possibilities for therapeutic application

C Goudet, V Binet, L Prezeau, JP Pin - Drug Discovery Today: Therapeutic …, 2004 - Elsevier
The two main neurotransmitters, glutamate and GABA, as well as calcium ions, sweet taste
molecules and some pheromones, act on class-C G-protein-coupled receptors (GPCRs) …

The calcium‐sensing receptor and calcimimetics in blood pressure modulation

S Smajilovic, S Yano, R Jabbari… - British journal of …, 2011 - Wiley Online Library
Calcium is a crucial second messenger in the cardiovascular system. However, calcium may
also be an extracellular first messenger through a G‐protein‐coupled receptor that senses …

Cinacalcet hydrochloride

JAB Balfour, LJ Scott - Drugs, 2005 - Springer
Abstract▲ Oral cinacalcet hydrochloride (HCl)[Sensipar®, Mimpara®] is the first in a new
class of therapeutic agents, the calcimimetics, and has a novel mechanism of action. It …

Structural basis for activation and allosteric modulation of full-length calcium-sensing receptor

T Wen, Z Wang, X Chen, Y Ren, X Lu, Y Xing, J Lu… - Science …, 2021 - science.org
Calcium-sensing receptor (CaSR) is a class CG protein–coupled receptor (GPCR) that plays
an important role in calcium homeostasis and parathyroid hormone secretion. Here, we …

[HTML][HTML] Recent advances in understanding the extracellular calcium-sensing receptor

M Colella, A Gerbino, AM Hofer, S Curci - F1000Research, 2016 - ncbi.nlm.nih.gov
The extracellular calcium-sensing receptor (CaR), a ubiquitous class C G-protein-coupled
receptor (GPCR), is responsible for the control of calcium homeostasis in body fluids. It …

[HTML][HTML] Direct determination of multiple ligand interactions with the extracellular domain of the calcium-sensing receptor

C Zhang, Y Zhuo, HA Moniz, S Wang… - Journal of Biological …, 2014 - ASBMB
Numerous in vivo functional studies have indicated that the dimeric extracellular domain
(ECD) of the CaSR plays a crucial role in regulating Ca 2+ homeostasis by sensing Ca 2+ …

Allosteric activation of the CaR by l-amino acids

B Kobilka - Proceedings of the National Academy of …, 2000 - National Acad Sciences
Gprotein-coupled receptors (GPCRs) serve as cellular sensors for a broad range of
stimulants including photons, odorants, hormones, neurotransmitters, and ions. The studies …