Discovery of a novel small molecule agonist scaffold for the APJ receptor

[Display omitted] The apelinergic system includes a series of endogenous peptides apelin, ELABELA/TODDLER and their 7-transmembrane G-protein coupled apelin receptor (APJ, AGTRL-1, APLNR). The APJ receptor is an attractive therapeutic target because of its involvement in cardiovascular diseases and...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2016-08, Vol.24 (16), p.3758-3770
Hauptverfasser:	Narayanan, Sanju, Maitra, Rangan, Deschamps, Jeffery R., Bortoff, Katherine, Thomas, James B., Zhang, Yanyan, Warner, Keith, Vasukuttan, Vineetha, Decker, Ann, Runyon, Scott P.
Format:	Artikel
Sprache:	eng
Schlagworte:	AGTRL1 Animals Apelin Apelin Receptors APJ small molecule agonist APLNR Cell Line Crystallography, X-Ray Drug Discovery Humans Proton Magnetic Resonance Spectroscopy Pyrazole Rats Receptors, G-Protein-Coupled - agonists Small Molecule Libraries Spectrometry, Mass, Electrospray Ionization Structure-Activity Relationship
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