Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.
Amino Acid Sequence
Animals
Apelin Receptors
/ agonists
Binding Sites
Blood Pressure
/ drug effects
Computational Biology
Heart
/ drug effects
Humans
Intercellular Signaling Peptides and Proteins
/ chemistry
Ligands
Male
Peptide Hormones
/ chemistry
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
14 01 2021
14 01 2021
Historique:
pubmed:
23
12
2020
medline:
9
3
2021
entrez:
22
12
2020
Statut:
ppublish
Résumé
ELABELA (ELA) is the second endogenous ligand of the apelin receptor (APJ). Although apelin-13 and ELA both target APJ, there is limited information on structure-activity relationship (SAR) of ELA. In the present work, we identified the shortest bioactive C-terminal fragment ELA23-32, which possesses high affinity for APJ (
Identifiants
pubmed: 33350824
doi: 10.1021/acs.jmedchem.0c01547
doi:
Substances chimiques
Apelin Receptors
0
Intercellular Signaling Peptides and Proteins
0
Ligands
0
Peptide Hormones
0
apelin-13 peptide
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
602-615Subventions
Organisme : CIHR
ID : FDN-148413
Pays : Canada
Organisme : CIHR
ID : FDN-148431
Pays : Canada