Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells.
Journal
Communications biology
ISSN: 2399-3642
Titre abrégé: Commun Biol
Pays: England
ID NLM: 101719179
Informations de publication
Date de publication:
27 11 2020
27 11 2020
Historique:
received:
15
05
2020
accepted:
03
11
2020
entrez:
28
11
2020
pubmed:
29
11
2020
medline:
24
6
2021
Statut:
epublish
Résumé
To study the localisation of G protein-coupled receptors (GPCR) in their native cellular environment requires their visualisation through fluorescent labelling. To overcome the requirement for genetic modification of the receptor or the limitations of dissociable fluorescent ligands, here we describe rational design of a compound that covalently and selectively labels a GPCR in living cells with a fluorescent moiety. We designed a fluorescent antagonist, in which the linker incorporated between pharmacophore (ZM241385) and fluorophore (sulfo-cyanine5) is able to facilitate covalent linking of the fluorophore to the adenosine A
Identifiants
pubmed: 33247190
doi: 10.1038/s42003-020-01451-w
pii: 10.1038/s42003-020-01451-w
pmc: PMC7695831
doi:
Substances chimiques
ADORA2A protein, human
0
Affinity Labels
0
Fluorescent Dyes
0
Ligands
0
Receptor, Adenosine A2A
0
Receptors, G-Protein-Coupled
0
Triazines
0
Triazoles
0
ZM 241385
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
722Subventions
Organisme : Medical Research Council
ID : MR/N020081/1
Pays : United Kingdom
Organisme : Department of Health
Pays : United Kingdom
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