Allosteric modulators of the extracellular calcium receptor.
Drug Discov Today Technol
; 10(2): e277-84, 2013.
Article
em En
| MEDLINE
| ID: mdl-24050279
ABSTRACT
The extracellular calcium receptor (CaR) is a Family C G protein-coupled receptor that controls systemic Ca2+ homeostasis, largely by regulating the secretion of parathyroid hormone (PTH). Ligands that activate the CaR have been termed calcimimetics and are classified as either Type I (agonists) or Type II (allosteric activators) and effectively inhibit the secretion of PTH. CaR antagonists have been termed calcilytics and all act allosterically to stimulate secretion of PTH. The calcimimetic cinacalcet has been approved for treating parathyroid cancer and secondary hyperparathyroidism in patients on renal replacement therapy. Cinacalcet was the first allosteric modulator of a G proteincoupled receptor to achieve regulatory approval. This review will focus on the technologies used to discover and develop allosterically acting calcimimetics and calcilytics as novel therapies for bone and mineral-related disorders.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Doenças Ósseas
/
Receptores de Detecção de Cálcio
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Drug Discov Today Technol
Ano de publicação:
2013
Tipo de documento:
Article