Cholesterol increases kinetic, energetic, and mechanical stability of the human β_2-adrenergic receptor

摘要

The human β_2-adrenergic receptor (β_2AR), one of the best-characterized G protein-coupled receptors (GPCRs), belongs to class A GPCRs and is expressed in pulmonary and cardiac myo-cyte tissue. Together with its close relative β_1AR, β_2AR senses adrenalin in bronchial vasculature and noradrenalin in cardiac muscle. The implication in a broad spectrum of diseases, such as asthma or heart failure, makes β_2AR a potential therapeutic target. Several crystal structures of β_2AR have been determined during the last years (1), providing unique insights into the structure-function relationship of GPCRs.