Fenoprofen-An Old Drug Rediscovered as a Biased Allosteric Enhancer for Melanocortin Receptors.
Melanocortin receptors
allosteric enhancer
biased signaling
drug repurposing
naturally occurring mutation
Journal
ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337
Informations de publication
Date de publication:
20 03 2019
20 03 2019
Historique:
pubmed:
1
9
2018
medline:
7
3
2020
entrez:
1
9
2018
Statut:
ppublish
Résumé
It is time-consuming and costly to bring new drugs to market, making it necessary and urgent to exploit existing drugs for new uses. Recently, fenoprofen was demonstrated as an allosteric modulator at melanocortin receptors (MCRs), although the exact mode of action has not been clarified. MCRs regulate multiple functions, including pigmentation, adrenal steroidogenesis, inflammation, energy homeostasis, and exocrine gland secretion. In this study, we showed that fenoprofen failed to displace the orthosteric agonist Nle
Identifiants
pubmed: 30168706
doi: 10.1021/acschemneuro.8b00347
doi:
Substances chimiques
Anti-Inflammatory Agents, Non-Steroidal
0
Anti-Obesity Agents
0
Receptors, Melanocortin
0
Fenoprofen
RA33EAC7KY
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM