Insights into the Interaction of LVV-Hemorphin-7 with Angiotensin II Type 1 Receptor.
AT1R
AngII
LVV-hemorphin-7
NanoBRET
PAM
molecular docking
molecular dynamics
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:
28 Dec 2020
28 Dec 2020
Historique:
received:
29
10
2020
revised:
17
12
2020
accepted:
24
12
2020
entrez:
31
12
2020
pubmed:
1
1
2021
medline:
8
9
2021
Statut:
epublish
Résumé
Hemorphins are known for their role in the control of blood pressure. Recently, we revealed the positive modulation of the angiotensin II (AngII) type 1 receptor (AT1R) by LVV-hemorphin-7 (LVV-H7) in human embryonic kidney (HEK293) cells. Here, we examined the molecular binding behavior of LVV-H7 on AT1R and its effect on AngII binding using a nanoluciferase-based bioluminescence resonance energy transfer (NanoBRET) assay in HEK293FT cells, as well as molecular docking and molecular dynamics (MD) studies. Saturation and real-time kinetics supported the positive effect of LVV-H7 on the binding of AngII. While the competitive antagonist olmesartan competed with AngII binding, LVV-H7 slightly, but significantly, decreased AngII's k
Identifiants
pubmed: 33379211
pii: ijms22010209
doi: 10.3390/ijms22010209
pmc: PMC7795518
pii:
doi:
Substances chimiques
Hemoglobins
0
Peptide Fragments
0
Receptor, Angiotensin, Type 1
0
Angiotensin II
11128-99-7
LVV-hemorphin-7
75808-66-1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : United Arab Emirates University
ID : 31R235 and 31S243
Organisme : Australian Research Council
ID : LP160100857
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