Selectivity in agonist and antagonist binding to Serotonin
Binding Sites
Drug Discovery
GTP-Binding Proteins
/ metabolism
Hydrogen-Ion Concentration
Protein Binding
Receptor, Serotonin, 5-HT1A
/ metabolism
Receptors, G-Protein-Coupled
/ metabolism
Serotonin 5-HT1 Receptor Agonists
/ metabolism
Serotonin 5-HT1 Receptor Antagonists
/ metabolism
Urea
/ pharmacology
Agonist
Antagonist
G-protein coupling
G-protein inactivation
GPCR
serotonin(1A) receptor
Journal
Biochimica et biophysica acta. Biomembranes
ISSN: 1879-2642
Titre abrégé: Biochim Biophys Acta Biomembr
Pays: Netherlands
ID NLM: 101731713
Informations de publication
Date de publication:
01 06 2020
01 06 2020
Historique:
received:
20
01
2020
revised:
04
03
2020
accepted:
05
03
2020
pubmed:
12
3
2020
medline:
21
8
2020
entrez:
12
3
2020
Statut:
ppublish
Résumé
G protein-coupled receptors (GPCRs) constitute the largest superfamily of membrane proteins in higher eukaryotes, and facilitate information transfer from the extracellular environment to the cellular interior upon activation by ligands. Their role in diverse signaling processes makes them an attractive choice as drug targets. GPCRs are coupled to heterotrimeric G-proteins which represent an important interface through which signal transduction occurs across the plasma membrane upon activation by ligands. To obtain further insight into the molecular details of interaction of G-proteins with GPCRs, in this work, we explored the selectivity of binding of specific agonists and antagonists to the serotonin
Identifiants
pubmed: 32156647
pii: S0005-2736(20)30090-0
doi: 10.1016/j.bbamem.2020.183265
pii:
doi:
Substances chimiques
Receptors, G-Protein-Coupled
0
Serotonin 5-HT1 Receptor Agonists
0
Serotonin 5-HT1 Receptor Antagonists
0
Receptor, Serotonin, 5-HT1A
112692-38-3
Urea
8W8T17847W
GTP-Binding Proteins
EC 3.6.1.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
183265Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.