A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the
Journal
Molecular pharmacology
ISSN: 1521-0111
Titre abrégé: Mol Pharmacol
Pays: United States
ID NLM: 0035623
Informations de publication
Date de publication:
06 2020
06 2020
Historique:
received:
23
10
2019
accepted:
18
03
2020
pubmed:
3
4
2020
medline:
4
8
2020
entrez:
3
4
2020
Statut:
ppublish
Résumé
G protein-coupled receptor (GPCR) kinases (GRKs) play a key role in terminating signals initiated by agonist-bound GPCRs. However, chronic stimulation of GPCRs, such as that which occurs during heart failure, leads to the overexpression of GRKs and maladaptive downregulation of GPCRs on the cell surface. We previously reported the discovery of potent and selective families of GRK inhibitors based on either the paroxetine or
Identifiants
pubmed: 32234810
pii: mol.119.118661
doi: 10.1124/mol.119.118661
pmc: PMC7237867
doi:
Substances chimiques
GSK180736A
0
Indazoles
0
OPRM1 protein, human
0
Pyrimidines
0
Receptors, Opioid, mu
0
Paroxetine
41VRH5220H
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
392-401Subventions
Organisme : NIGMS NIH HHS
ID : R01 GM117425
Pays : United States
Organisme : NHLBI NIH HHS
ID : R01 HL071818
Pays : United States
Organisme : NHLBI NIH HHS
ID : R01 HL122416
Pays : United States
Informations de copyright
Copyright © 2020 by The American Society for Pharmacology and Experimental Therapeutics.
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