Calcium-sensing receptor 20 years later
TI Alfadda, AMA Saleh, P Houillier… - American Journal of …, 2014 - journals.physiology.org
The calcium-sensing receptor (CaSR) has played an important role as a target in the
treatment of a variety of disease states over the past 20 plus years. In this review, we give an …
treatment of a variety of disease states over the past 20 plus years. In this review, we give an …
Molecular insights into allosteric modulation of Class CG protein-coupled receptors
K Leach, KJ Gregory - Pharmacological Research, 2017 - Elsevier
Class CG protein-coupled receptors (GPCRs) recognise diverse extracellular stimuli and are
highly tractable drug targets for a host of different psychiatric, neurological and metabolic …
highly tractable drug targets for a host of different psychiatric, neurological and metabolic …
[HTML][HTML] Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor
Drugs that allosterically target the human calcium-sensing receptor (CaSR) have substantial
therapeutic potential, but are currently limited. Given the absence of high-resolution …
therapeutic potential, but are currently limited. Given the absence of high-resolution …
[HTML][HTML] A novel calcimimetic agent, evocalcet (MT-4580/KHK7580), suppresses the parathyroid cell function with little effect on the gastrointestinal tract or CYP isozymes in vivo …
T Kawata, S Tokunaga, M Murai, N Masuda… - PLoS …, 2018 - journals.plos.org
Cinacalcet hydrochloride (cinacalcet), an oral calcimimetic agent has been widely used for
the management of secondary hyperparathyroidism (SHPT) in chronic kidney disease …
the management of secondary hyperparathyroidism (SHPT) in chronic kidney disease …
[HTML][HTML] The different facets of extracellular calcium sensors: old and new concepts in calcium-sensing receptor signalling and pharmacology
The current interest of the scientific community for research in the field of calcium sensing in
general and on the calcium-sensing Receptor (CaR) in particular is demonstrated by the still …
general and on the calcium-sensing Receptor (CaR) in particular is demonstrated by the still …
[HTML][HTML] Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine
X Zhang, T Jin, N Shi, L Yao, X Yang, C Han… - Frontiers in …, 2019 - frontiersin.org
Pancreatic acinar cells require high rates of amino acid uptake for digestive enzyme
synthesis, but excessive concentrations can trigger acute pancreatitis (AP) by mechanisms …
synthesis, but excessive concentrations can trigger acute pancreatitis (AP) by mechanisms …
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 …
controls systemic Ca2+ homeostasis, largely by regulating the secretion of parathyroid …
[HTML][HTML] G-protein coupled receptor targeting on myeloid cells in atherosclerosis
EPC Van der Vorst, LJF Peters, M Müller… - Frontiers in …, 2019 - frontiersin.org
Atherosclerosis, the underlying cause of the majority of cardiovascular diseases (CVDs), is a
lipid-driven, inflammatory disease of the large arteries. Gold standard therapy with statins …
lipid-driven, inflammatory disease of the large arteries. Gold standard therapy with statins …
[HTML][HTML] NPS-2143 (hydrochloride) inhibits melanoma cancer cell proliferation and induces autophagy and apoptosis
S Wang, L Qiu, H Song, N Dang - médecine/sciences, 2018 - medecinesciences.org
Melanoma is a common and aggressive skin cancer caused by the oncogenic
transformation of melanocytes. NPS-2143 (hydrochloride) is a calcification drug that acts as …
transformation of melanocytes. NPS-2143 (hydrochloride) is a calcification drug that acts as …
Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism
PM Wehn, PE Harrington, TJ Carlson, J Davis… - Bioorganic & medicinal …, 2013 - Elsevier
A series of urea based calcimimetics was optimized for potency and oral bioavailability.
Crucial to this process was overcoming the poor pharmacokinetic properties of lead thiazole …
Crucial to this process was overcoming the poor pharmacokinetic properties of lead thiazole …