Discovery of a calcimimetic with differential effects on parathyroid hormone and calcitonin secretion

C Henley, Y Yang, J Davis, JYL Lu, S Morony… - … of Pharmacology and …, 2011 - ASPET
Calcimimetics are positive allosteric modulators to the calcium-sensing receptor (CaSR).
Activation of the CaSR inhibits the secretion of parathyroid hormone (PTH), stimulates the …

Calcimimetic and calcilytic drugs: feats, flops, and futures

EF Nemeth, WG Goodman - Calcified Tissue International, 2016 - Springer
The actions of extracellular Ca 2+ in regulating parathyroid gland and kidney functions are
mediated by the extracellular calcium receptor (CaR), a G protein-coupled receptor. The …

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 …

Clinical utility of calcimimetics targeting the extracellular calcium-sensing receptor (CaSR)

EM Brown - Biochemical pharmacology, 2010 - Elsevier
Calcimimetics, which activate the extracellular calcium (Cao2+)-sensing receptor in the
parathyroid and other tissues participating in Cao2+ homeostasis, were the first described …

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 …

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 …

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 …

Relationship between parathyroid calcium-sensing receptor expression and potency of the calcimimetic, cinacalcet, in suppressing parathyroid hormone secretion in …

T Kawata, Y Imanishi, K Kobayashi… - European journal of …, 2005 - academic.oup.com
Cinacalcet HCl, an allosteric modulator of the calcium-sensing receptor (CaR), has recently
been approved for the treatment of secondary hyperparathyroidism in patients with chronic …

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 …

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 …