Cryo-electron microscopy structure of the glucagon receptor with a dual-agonist peptide.
G protein–coupled receptor (GPCR)
GLP-1 receptor
cryo-electron microscopy
dual agonist
glucagon
glucagon receptor
glucagon-like peptide-1 receptor
metabolic disorder
peptide 15 (P15)
single particle analysis
structural biology
structure-function
Journal
The Journal of biological chemistry
ISSN: 1083-351X
Titre abrégé: J Biol Chem
Pays: United States
ID NLM: 2985121R
Informations de publication
Date de publication:
10 07 2020
10 07 2020
Historique:
received:
09
04
2020
revised:
30
04
2020
pubmed:
7
5
2020
medline:
14
1
2021
entrez:
7
5
2020
Statut:
ppublish
Résumé
Unimolecular dual agonists of the glucagon (GCG) receptor (GCGR) and glucagon-like peptide-1 receptor (GLP-1R) are a new class of drugs that are potentially superior to GLP-1R-specific agonists for the management of metabolic disease. The dual-agonist, peptide 15 (P15), is a glutamic acid 16 analog of GCG with GLP-1 peptide substitutions between amino acids 17 and 24 that has potency equivalent to those of the cognate peptide agonists at the GCGR and GLP-1R. Here, we have used cryo-EM to solve the structure of an active P15-GCGR-G
Identifiants
pubmed: 32371397
pii: S0021-9258(17)48955-1
doi: 10.1074/jbc.RA120.013793
pmc: PMC7363120
doi:
Substances chimiques
GLP1R protein, human
0
Glucagon-Like Peptide-1 Receptor
0
Peptides
0
Receptors, Glucagon
0
Banques de données
PDB
['6LMK', '5VAI']
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
9313-9325Informations de copyright
© 2020 Chang et al.
Déclaration de conflit d'intérêts
Conflict of interest—The authors declare that they have no conflicts of interest with the contents of this article.
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