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Cancer-Associated Mutations of the Adenosine A2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions.

Molecules (Basel, Switzerland) - 22 Jul 2022

Feng Chenlin, Wang Xuesong, Jespers Willem, Liu Rongfang, Zamarbide Losada Sofía Denise, Gorostiola González Marina, van Westen Gerard J P, Danen Erik H J, Heitman Laura H

Abstract excerpt

The adenosine A2A receptor (A2AAR) is a class A G-protein-coupled receptor (GPCR). It is an immune checkpoint in the tumor micro-environment and has become an emerging target for cancer treatment. In this study, we aimed to explore the effects of cancer-patient-derived A2AAR mutations on ligand binding and receptor functions. The wild-type A2AAR and 15 mutants identified by Genomic Data Commons (GDC) in human...

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PMID: 35897852
DOI: 10.3390/molecules27154676
PMCID: PMC9331671

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