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 - Elsevier
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 …

Biased and allosteric modulation of bone cell-expressing G protein-coupled receptors as a novel approach to osteoporosis therapy

A Kalinkovich, G Livshits - Pharmacological Research, 2021 - Elsevier
On the cellular level, osteoporosis (OP) is a result of imbalanced bone remodeling, in which
osteoclastic bone resorption outcompetes osteoblastic bone formation. Currently available …

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 …

Symmetric activation and modulation of the human calcium-sensing receptor

J Park, H Zuo, A Frangaj, Z Fu, LY Yen… - Proceedings of the …, 2021 - National Acad Sciences
The human extracellular calcium-sensing (CaS) receptor controls plasma Ca2+ levels and
contributes to nutrient-dependent maintenance and metabolism of diverse organs. Allosteric …

Therapeutic opportunities of targeting allosteric binding sites on the calcium-sensing receptor

J Diao, A DeBono, TM Josephs, JE Bourke… - ACS Pharmacology & …, 2021 - ACS Publications
The CaSR is a class CG protein-coupled receptor (GPCR) that acts as a multimodal
chemosensor to maintain diverse homeostatic functions. The CaSR is a clinical therapeutic …

The effect of high-fat diet-induced obesity on the expression of nutrient chemosensors in the mouse stomach and the gastric ghrelin cell

M Nunez-Salces, H Li, S Christie, AJ Page - Nutrients, 2020 - mdpi.com
The stomach is the primary source of the orexigenic and adiposity-promoting hormone,
ghrelin. There is emerging evidence on the nutrient-mediated modulation of gastric ghrelin …

Structural mechanism of cooperative regulation of calcium-sensing receptor-mediated cellular signaling

X Deng, Y Xin, CL Miller, D Hamelberg… - Current opinion in …, 2020 - Elsevier
Calcium-sensing receptors (CaSRs) play a central role in regulating extracellular calcium
(Ca 2+) homeostasis and many (patho) physiological processes. This regulation is primarily …

Ca2+-sensing receptor-TRP channel-mediated Ca2+ signaling: functional diversity and pharmacological complexity

KC Wu, IL Leong, YM Leung - European Journal of Pharmacology, 2024 - Elsevier
Abstract The Ca 2+-sensing receptor (CaSR) is a G-protein-coupled receptor activated by
elevated concentrations of extracellular Ca 2+, and was initially known for its regulation of …

Development of AC265347‐Inspired Calcium‐Sensing Receptor Ago‐Positive Allosteric Modulators

LV Dinh, A DeBono, AN Keller, TM Josephs… - …, 2021 - Wiley Online Library
The calcium‐sensing receptor (CaSR) is a clinical target in the treatment of
hyperparathyroidism and related diseases. However, clinical use of approved CaSR …

Calcium-Sensing Receptor Negative Allosteric Modulators Oppose Contraction of Mouse Airways

J Diao, M Lam, KJ Gregory, K Leach… - American Journal of …, 2023 - atsjournals.org
Asthma is a heterogeneous chronic airway disease with an unmet need for improved
therapeutics in uncontrolled severe disease. The calcium-sensing receptor (CaSR) is a G …