Ψ and χ Angle Constrains at the C-Terminus Trp Position of the Melanotropin Tetrapeptide Ac-His-d-Phe-Arg-Trp-NH 2 Lead to Potent and Selective Agonists at hMC1R and hMC4R

Melanocortin receptors (MCRs) are a family of G protein-coupled receptors that regulate important physiological functions. Yet, drug development targeting MCRs is hindered by potential side effects due to a lack of receptor subtype-selective ligands with bioavailability. Here, we report novel synthe...

Ausführliche Beschreibung

Bibliographische Detailangaben

Veröffentlicht in:	Journal of medicinal chemistry 2023-05, Vol.66 (10), p.6715-6724
Hauptverfasser:	Zhou, Yang, Mowlazadeh Haghighi, Saghar, Sawyer, Jonathon R, Hruby, Victor J, Cai, Minying
Format:	Artikel
Sprache:	eng
Schlagworte:	Melanocyte-Stimulating Hormones Molecular Conformation Molecular Docking Simulation Receptor, Melanocortin, Type 4 - metabolism Receptors, Melanocortin Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!