Cholesterol Dependent Activity of the Adenosine A_2A Receptor Is Modulated via the Cholesterol Consensus Motif.

ABSTRACT:

Background

Membrane cholesterol dysregulation has been shown to alter the activity of the adenosine A_2A receptor (A_2AR), a G protein-coupled receptor, thereby implicating cholesterol levels in diseases such as Alzheimer's and Parkinson's. A limited number of A_2AR crystal structures show the receptor interacting with cholesterol, as such molecular simulations are often used to predict cholesterol interaction sites.

Methods

Here, we use experimental methods to determine whether a specific interaction between amino acid side chains in the cholesterol consensus motif (CCM) of full length, wild-type human A_2AR, and cholesterol modulates activity of the receptor by testing the effects of mutational changes on functional consequences, inc

SUBMITTER: McGraw C 

PROVIDER: S-EPMC9182133 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature