Orthosteric, Allosteric and Biased Signalling at the Relaxin-3 Receptor RXFP3.
Neurochem Res
; 41(3): 610-9, 2016 Mar.
Article
em En
| MEDLINE
| ID: mdl-26294284
ABSTRACT
Relaxin-3 is a neuropeptide that has roles in stress, memory and appetite regulation. The peptide acts on its cognate receptor RXFP3 to induce coupling to inhibitory G proteins to inhibit adenylyl cyclase and activate MAP-kinases such as ERK1/2, p38MAPK and JNK. Other relaxin family peptides can activate the receptor to produce alternative patterns of signalling and there is an allosteric modulator 135PAM1 that displays probe-selectivity. There are now a variety of selective peptide agonists and antagonists that will assist in the determination of the physiological roles of the relaxin-RXFP3 system and its potential as a drug target.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores de Peptídeos
/
Receptores Acoplados a Proteínas G
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Neurochem Res
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Austrália