Novel non-peptide uracil-derived human gonadotropin-releasing hormone receptor antagonists

Gonadotropin-releasing hormone (GnRH) is the main regulator of the reproductive system, acting on gonadotropic cells by binding to the GnRH1 receptor (GnRH1R). Traditionally, therapies targeting this receptor have relied on peptide modulators, which required subcutaneous or intramuscular injections....

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Veröffentlicht in:	European journal of medicinal chemistry 2024-12, Vol.279, p.116903, Article 116903
Hauptverfasser:	Ciceri, Samuele, Fassi, Enrico M.A., Vezzoli, Valeria, Bonomi, Marco, Colombo, Diego, Ferraboschi, Patrizia, Grazioso, Giovanni, Grisenti, Paride, Villa, Stefania, Castellano, Carlo, Meneghetti, Fiorella
Format:	Artikel
Sprache:	eng
Schlagworte:	Atropisomerism Cytosine Cytosine derivative Dose-Response Relationship, Drug Elagolix GnRH modulators Humans MD simulations Molecular Docking Simulation Molecular Dynamics Simulation Molecular Structure NMR spectroscopy Quanto-mechanics Receptors, LHRH - antagonists & inhibitors Receptors, LHRH - metabolism SC-XRD Structure-Activity Relationship Thio-uracil derivative Uracil - analogs & derivatives Uracil - chemical synthesis Uracil - chemistry Uracil - pharmacology
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