GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A<sub>2A</sub> Adenosine Receptor
Anna Shiriaeva, Daejin Park, Gyudong Kim, Yoonji Lee, Xiyan Hou, Dnyandev B. Jarhad, Gibae Kim, Jinha Yu, Young Eum Hyun, Woomi Kim, Zhan‐Guo Gao, Kenneth A. Jacobson, Gye Won Han, Raymond C. Stevens, Lak Shin Jeong, Sun Choi, Vadim Cherezov
Abstract
AR exosite. Structural analysis revealed that the introduced thiophene modification restricted receptor conformational rearrangements required for subsequent activation. This approach can expand the repertoire of adenosine receptor antagonists that can be designed based on available agonist scaffolds.
Topics & Concepts
AgonistChemistryAdenosineAdenosine receptorAntagonistG protein-coupled receptorReceptorPartial agonistStereochemistryPharmacologyBiochemistryMedicineAdenosine and Purinergic SignalingReceptor Mechanisms and SignalingPharmacological Receptor Mechanisms and Effects