Cryo-EM structure of the human adenosine A_2B receptor-G_s signaling complex.

ABSTRACT: The human adenosine A_2B receptor (A_2BR) is a class A G protein-coupled receptor that is involved in several major physiological and pathological processes throughout the body. A_2BR recognizes its ligands adenosine and NECA with relatively low affinity, but the detailed mechanism for its ligand recognition and signaling is still elusive. Here, we present two structures determined by cryo-electron microscopy of A_2BR bound to its agonists NECA and BAY60-6583, each coupled to an engineered G_s protein. The structures reveal conserved orthosteric binding pockets with subtle differences, whereas the selectivity or specificity can mainly be attributed to regions extended from the orthosteric pocket. We also found that BAY60-6583 occupies a sec

SUBMITTER: Chen Y 

PROVIDER: S-EPMC9788782 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature