Article
Allosteric Antagonism of the A2A Adenosine Receptor by a Series of Bitopic Ligands.
Cells - 12 May 2020
Gao Zhan-Guo, Toti Kiran S, Campbell Ryan, Suresh R Rama, Yang Huijun, Jacobson Kenneth A
Abstract excerpt
Allosteric antagonism by bitopic ligands, as reported for many receptors, is a distinct modulatory mechanism. Although several bitopic A2A adenosine receptor (A2AAR) ligand classes were reported as pharmacological tools, their receptor binding and functional antagonism patterns, i.e., allosteric or competitive, were not well characterized. Therefore, here we systematically characterized A2AAR binding and...
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