In Vitro Analyses of Spinach-Derived Opioid Peptides, Rubiscolins: Receptor Selectivity and Intracellular Activities through G Protein- and β-Arrestin-Mediated Pathways.
GTP-Binding Proteins
/ metabolism
Gene Expression Regulation
/ drug effects
HEK293 Cells
Humans
Molecular Structure
Opioid Peptides
/ chemistry
Peptide Fragments
/ chemistry
Receptors, Opioid, delta
/ agonists
Receptors, Opioid, mu
/ metabolism
Ribulose-Bisphosphate Carboxylase
/ chemistry
Signal Transduction
/ drug effects
Spinacia oleracea
/ chemistry
beta-Arrestins
/ metabolism
G-protein-biased agonist
analgesic
opioid peptide
rubiscolins
δ opioid receptor
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
08 Oct 2021
08 Oct 2021
Historique:
received:
17
09
2021
revised:
29
09
2021
accepted:
30
09
2021
entrez:
13
10
2021
pubmed:
14
10
2021
medline:
17
11
2021
Statut:
epublish
Résumé
Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists are preferable as opioid analgesics. Rubiscolins, the spinach-derived naturally occurring opioid peptides, are selective δ opioid receptor agonists, and their p.o. administration exhibits antinociceptive effects. Although the potency and effect of rubiscolins as G-protein-biased molecules are partially confirmed, their in vitro profiles remain unclear. We, therefore, evaluated the properties of rubiscolins, in detail, through several analyses, including the CellKey
Identifiants
pubmed: 34641621
pii: molecules26196079
doi: 10.3390/molecules26196079
pmc: PMC8513079
pii:
doi:
Substances chimiques
Opioid Peptides
0
Peptide Fragments
0
Receptors, Opioid, delta
0
Receptors, Opioid, mu
0
beta-Arrestins
0
rubiscolin 5
0
rubiscolin 6
0
GTP-Binding Proteins
EC 3.6.1.-
Ribulose-Bisphosphate Carboxylase
EC 4.1.1.39
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : JSPS KAKENHI
ID : JP18K07404, JP18K08858, JP21K06584
Organisme : The National Cancer Center Research and Development Fund
ID : 29-A-48
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