Design, synthesis and evaluation of unnatural peptides as T1R2/T1R3 PAMs.
Enhancer
G protein-coupled receptor
PAM
T1R2/T1R3
Unnatural peptide
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 04 2020
15 04 2020
Historique:
received:
21
11
2019
revised:
21
01
2020
accepted:
24
01
2020
pubmed:
18
2
2020
medline:
1
5
2021
entrez:
18
2
2020
Statut:
ppublish
Résumé
The sweet receptor T1R2/T1R3 is a member of G protein-coupled receptor family and recognizes diverse natural and synthetic sweeteners. Previously, we reported a novel class of positive allosteric modulators (PAMs) of T1R2/T1R3 comprising an unnatural tripeptide structure. We classified the structure of these PAMs into three parts: "head", "linker" and "tail". Here, we report the design, synthesis and evaluation of various tail structures to obtain highly active unnatural peptide structure of PAM. In conclusion, we discovered the novel unnatural tetrapeptide with highly potent PAM activity on T1R2/T1R3 in a cell-based assay system.
Identifiants
pubmed: 32063432
pii: S0960-894X(20)30063-9
doi: 10.1016/j.bmcl.2020.127000
pii:
doi:
Substances chimiques
Peptides
0
Receptors, G-Protein-Coupled
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
127000Informations de copyright
Copyright © 2020 Elsevier Ltd. 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.