International union of basic and clinical pharmacology. CVIII. Calcium-sensing receptor nomenclature, pharmacology, and function

K Leach, FM Hannan, TM Josephs, AN Keller… - Pharmacological …, 2020 - ASPET
The calcium-sensing receptor (CaSR) is a class CG protein–coupled receptor that responds
to multiple endogenous agonists and allosteric modulators, including divalent and trivalent …

Engendering biased signalling from the calcium‐sensing receptor for the pharmacotherapy of diverse disorders

K Leach, PM Sexton, A Christopoulos… - British journal of …, 2014 - Wiley Online Library
The human calcium‐sensing receptor (CaSR) is widely expressed in the body, where its
activity is regulated by multiple orthosteric and endogenous allosteric ligands. Each ligand …

Calcium-sensing receptor (CaSR): pharmacological properties and signaling pathways

AD Conigrave, DT Ward - Best practice & research Clinical endocrinology & …, 2013 - Elsevier
In this article we consider the mechanisms by which the calcium-sensing receptor (CaSR)
induces its cellular responses via the control (activation or inhibition) of signaling pathways …

Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho) physiological bias

K Leach, AD Conigrave, PM Sexton… - Trends in …, 2015 - cell.com
The calcium-sensing receptor (CaSR) is a widely expressed G protein-coupled receptor
(GPCR) that mediates numerous tissue-specific functions. Its multiple ligands and diverse …

Structural basis for regulation of human calcium-sensing receptor by magnesium ions and an unexpected tryptophan derivative co-agonist

C Zhang, T Zhang, J Zou, CL Miller, R Gorkhali… - Science …, 2016 - science.org
Ca2+-sensing receptors (CaSRs) modulate calcium and magnesium homeostasis and many
(patho) physiological processes by responding to extracellular stimuli, including divalent …

Calcium-sensing receptor and associated diseases

GN Hendy, V Guarnieri, L Canaff - Progress in molecular biology and …, 2009 - Elsevier
The calcium-sensing receptor (CASR) is expressed in parathyroid hormone (PTH)-secreting
cells of the parathyroid gland and cells lining the renal tubule. The activated CASR …

Signaling through the extracellular calcium-sensing receptor (CaSR)

B Chakravarti, N Chattopadhyay, EM Brown - Calcium signaling, 2012 - Springer
The extracellular calcium (Ca _ o^ 2+)-sensing receptor (CaSR) was the first GPCR
identified whose principal physiological ligand is an ion, namely extracellular Ca 2+. It …

[HTML][HTML] Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor

K Leach, KJ Gregory, I Kufareva, E Khajehali, AE Cook… - Cell research, 2016 - nature.com
Drugs that allosterically target the human calcium-sensing receptor (CaSR) have substantial
therapeutic potential, but are currently limited. Given the absence of high-resolution …

Biased agonism of the calcium-sensing receptor

ARB Thomsen, M Hvidtfeldt, H Bräuner-Osborne - Cell calcium, 2012 - Elsevier
After the discovery of molecules modulating G protein-coupled receptors (GPCRs) that are
able to selectively affect one signaling pathway over others for a specific GPCR, thereby …

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor

AE Davey, K Leach, C Valant, AD Conigrave… - …, 2012 - academic.oup.com
The calcium-sensing receptor (CaSR) is a G protein-coupled receptor whose function can
be allosterically modulated in a positive or negative manner by calcimimetics or calcilytics …