Probe dependence of allosteric enhancers on the binding affinity of adenosine A
Journal
British journal of pharmacology
ISSN: 1476-5381
Titre abrégé: Br J Pharmacol
Pays: England
ID NLM: 7502536
Informations de publication
Date de publication:
04 2019
04 2019
Historique:
received:
25
07
2018
revised:
02
11
2018
accepted:
04
12
2018
pubmed:
16
1
2019
medline:
25
4
2020
entrez:
16
1
2019
Statut:
ppublish
Résumé
Adenosine is a local mediator that regulates a number of physiological and pathological processes via activation of adenosine A A Nano-luciferase (Nluc) BRET (NanoBRET) methodology was used. This used N-terminal Nluc-tagged A PD 81,723 and VCP171 elicited positive allosteric effects on the binding affinity of orthosteric agonists at both the rat and human A These results demonstrate the power of the NanoBRET ligand-binding approach to study the effect of allosteric ligands on the binding of fluorescent agonists to the adenosine A
Sections du résumé
BACKGROUND AND PURPOSE
Adenosine is a local mediator that regulates a number of physiological and pathological processes via activation of adenosine A
EXPERIMENTAL APPROACH
A Nano-luciferase (Nluc) BRET (NanoBRET) methodology was used. This used N-terminal Nluc-tagged A
KEY RESULTS
PD 81,723 and VCP171 elicited positive allosteric effects on the binding affinity of orthosteric agonists at both the rat and human A
CONCLUSIONS AND IMPLICATIONS
These results demonstrate the power of the NanoBRET ligand-binding approach to study the effect of allosteric ligands on the binding of fluorescent agonists to the adenosine A
Identifiants
pubmed: 30644086
doi: 10.1111/bph.14575
pmc: PMC6433648
doi:
Substances chimiques
Ligands
0
Purinergic P1 Receptor Agonists
0
Receptor, Adenosine A1
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
864-878Subventions
Organisme : British Heart Foundation
ID : PG/14/95/31248
Pays : United Kingdom
Organisme : Medical Research Council
ID : MR/N020081/1
Pays : United Kingdom
Informations de copyright
© 2019 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.
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