Membrane cholesterol depletion reduces downstream signaling activity of the adenosine A_2A receptor.

ABSTRACT: Cholesterol has been shown to modulate the activity of multiple G Protein-coupled receptors (GPCRs), yet whether cholesterol acts through specific interactions, indirectly via modifications to the membrane, or via both mechanisms is not well understood. High-resolution crystal structures of GPCRs have identified bound cholesterols; based on a β₂-adrenergic receptor (β₂AR) structure bound to cholesterol and the presence of conserved amino acids in class A receptors, the cholesterol consensus motif (CCM) was identified. Here in mammalian cells expressing the adenosine A_2A receptor (A_2AR), ligand dependent production of cAMP is reduced following membrane cholesterol depletion with methyl-beta-cyclodextrin (MβCD), indicating that A_2AR sign

SUBMITTER: McGraw C 

PROVIDER: S-EPMC6383678 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature