Article
A2A and A2B adenosine receptors: The extracellular loop 2 determines high (A2A) or low affinity (A2B) for adenosine.
Biochemical pharmacology - 1 Feb 2020
De Filippo Elisabetta, Hinz Sonja, Pellizzari Veronica, Deganutti Giuseppe, El-Tayeb Ali, Navarro Gemma, Franco Rafael, Moro Stefano, Schiedel Anke C, Müller Christa E
Abstract excerpt
A2A and A2B adenosine receptors (ARs) are closely related G protein-coupled receptor subtypes, which represent important (potential) drug targets. Despite their almost identical binding sites for adenosine, A2AARs are activated by low (nanomolar) adenosine concentrations, while A2BARs require micromolar concentrations. In the present study, we exchanged the extracellular loop 2 (ECL2) of the human A2AAR for that...
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