Role of Cholesterol in Adenosine A2A Receptor Activity

G-protein coupled receptors (GPCRs) represent the largest family of membrane proteins in the living world, and serve key roles in cellular signaling to diverse stimuli. For this reason, GPCRs are the largest target of therapeutics on the market. Despite this importance, our understanding of the relationship between structure and function, including downstream signaling, is rather limited. Since the first human GPCR, β2-adrenergic receptor, was crystallized in 2007, a specific cholesterol binding site between helices I, II, III and IV - the cholesterol consensus motif (CCM) - was established, and as many as 25% of all class A GPCRs have been predicted to have a specific interaction with cholesterol.

http://ift.tt/2s0nmwT