Crystal structure of a constitutive active mutant of adenosine A_2A receptor.

ABSTRACT: The adenosine A_2A receptor (A_2AAR) is a prototypical member of the class A subfamily of G-protein-coupled receptors (GPCRs) that is widely distributed in various tissues and organs of the human body, and participates in many important signal-regulation processes. We have previously summarized a common activation pathway of class A GPCRs in which a series of conserved residues/motifs undergo conformational change during extracellular agonist binding and finally induce the coupling of intracellular G protein. Through this mechanism we have successfully predicted several novel constitutive active or inactive mutations for A_2AAR. To reveal the molecular mechanism of mutation-induced constitutive activity, we determined the structure of a typical mutant I92N com

SUBMITTER: Cui M 

PROVIDER: S-EPMC9067115 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature