Development of Generic G Protein Peptidomimetics Able to Stabilize Active State G
GPCRs
allosteric modulators
drug discovery
fragment screening
peptidomimetics
Journal
Angewandte Chemie (International ed. in English)
ISSN: 1521-3773
Titre abrégé: Angew Chem Int Ed Engl
Pays: Germany
ID NLM: 0370543
Informations de publication
Date de publication:
26 04 2021
26 04 2021
Historique:
revised:
05
02
2021
received:
05
01
2021
pubmed:
18
2
2021
medline:
7
8
2021
entrez:
17
2
2021
Statut:
ppublish
Résumé
G protein-coupled receptors (GPCRs) represent an important group of membrane proteins that play a central role in modern medicine. Unfortunately, conformational promiscuity hampers full therapeutic exploitation of GPCRs, since the largest population of the receptor will adopt a basal conformation, which subsequently challenges screens for agonist drug discovery programs. Herein, we describe a set of peptidomimetics able to mimic the ability of G proteins in stabilizing the active state of the β
Identifiants
pubmed: 33596327
doi: 10.1002/anie.202100180
doi:
Substances chimiques
Peptidomimetics
0
Receptors, G-Protein-Coupled
0
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
10247-10254Informations de copyright
© 2021 Wiley-VCH GmbH.
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