State-Targeting Stabilization of Adenosine A
G-protein coupled receptor
adenosine A2A receptor
computational protein design
de novo designed protein
fusion partner protein
protein stabilization
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
29 Nov 2021
29 Nov 2021
Historique:
received:
24
09
2021
revised:
19
11
2021
accepted:
23
11
2021
entrez:
10
12
2021
pubmed:
11
12
2021
medline:
27
1
2022
Statut:
epublish
Résumé
G-protein coupled receptors (GPCRs) are known for their low stability and large conformational changes upon transitions between multiple states. A widely used method for stabilizing these receptors is to make chimeric receptors by fusing soluble proteins (i.e., fusion partner proteins) into the intracellular loop 3 (ICL3) connecting the transmembrane helices 5 and 6 (TM5 and TM6). However, this fusion approach requires experimental trial and error to identify appropriate soluble proteins, residue positions, and linker lengths for making the fusion. Moreover, this approach has not provided state-targeting stabilization of GPCRs. Here, to rationally stabilize a class A GPCR, adenosine A
Identifiants
pubmed: 34884716
pii: ijms222312906
doi: 10.3390/ijms222312906
pmc: PMC8657880
pii:
doi:
Substances chimiques
Adenosine A2 Receptor Agonists
0
Ligands
0
Proteins
0
Receptor, Adenosine A2A
0
Recombinant Fusion Proteins
0
Adenosine
K72T3FS567
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Japan Society for the Promotion of Science
ID : 18H05420
Organisme : Japan Society for the Promotion of Science
ID : 18H05425
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