Mu-Opioid receptor biased ligands: A safer and painless discovery of analgesics?
Drug Discov Today
; 22(11): 1719-1729, 2017 11.
Article
em En
| MEDLINE
| ID: mdl-28743488
Biased activation of G-protein-coupled receptors (GPCRs) is shifting drug discovery efforts and appears promising for the development of safer drugs. The most effective analgesics to treat acute pain are agonists of the µ opioid receptor (µ-OR), a member of the GPCR superfamily. However, the analgesic use of opioid drugs, such as morphine, is hindered by adverse effects. Only a few µ-OR agonists have been reported to selectively activate the Gi over ß-arrestin signaling pathway, resulting in lower gastrointestinal dysfunction and respiratory suppression. Here, we discuss the strategies that led to the development of biased µ-OR agonists, and potential areas for improvement, with an emphasis on structural aspects of the ligand-receptor recognition process.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores Opioides mu
/
Descoberta de Drogas
/
Analgésicos Opioides
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Drug Discov Today
Assunto da revista:
FARMACOLOGIA
/
TERAPIA POR MEDICAMENTOS
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
México
País de publicação:
Reino Unido