Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist

[Display omitted] •Discovery of a novel class of thyrotropin receptor antagonists.•A highly potent compound with oral efficacy was identified.•Risk of mutagenicity of compounds strongly reduced.•Efficacy correlates with exposure after oral dosing. The thyrotropin receptor (TSH-R) regulates the thyro...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2023-04, Vol.84, p.117258-117258, Article 117258
Hauptverfasser:	Karstens, Willem F.J., M.B.P. Menge, Wiro, Martens, Gijs, op het Veld, Sanne J.N., Th.H. van Eupen, Jacobus, Demon, Marco, van Achterberg, Tanja A.E., Arisse-Thijssen, Monica J., Santegoeds-Lenssen, Ellen W.H., van der Lee, Miranda M.C., Ubink, Ruud, Arends, Roel J., Sesink, Aloys, Blomenröhr, Marion, Marco Timmers, C.
Format:	Artikel
Sprache:	eng
Schlagworte:	Autoantibodies GPCR-antagonist Graves Disease - drug therapy Graves’ disease Humans Receptors, G-Protein-Coupled Receptors, Thyrotropin - antagonists & inhibitors Small molecule antagonist Thyroid stimulating hormone receptor Thyrotropin - metabolism Thyrotropin receptor TSH-R antagonist
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