GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor

Modulators of the G protein-coupled A2A adenosine receptor (A2AAR) have been considered promising agents to treat Parkinson’s disease, inflammation, cancer, and central nervous system disorders. Herein, we demonstrate that a thiophene modification at the C8 position in the common adenine scaffold co...

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Veröffentlicht in:	Journal of medicinal chemistry 2022-09, Vol.65 (17), p.11648-11657
Hauptverfasser:	Shiriaeva, Anna, Park, Daejin, Kim, Gyudong, Lee, Yoonji, Hou, Xiyan, Jarhad, Dnyandev B., Kim, Gibae, Yu, Jinha, Hyun, Young Eum, Kim, Woomi, Gao, Zhan-Guo, Jacobson, Kenneth A., Han, Gye Won, Stevens, Raymond C., Jeong, Lak Shin, Choi, Sun, Cherezov, Vadim
Format:	Artikel
Sprache:	eng
Online-Zugang:	Volltext
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