Mutation of Asn293 to Asp in transmembrane helix VI abolishes agonist-induced but not constitutive activity of the beta(2)-adrenergic receptor.

Abstract excerpt

The beta(2)-adrenergic receptor has been shown to display significant constitutive activity (i.e., in the absence of agonist) in addition to agonist-induced activation. Various studies have suggested that a movement in transmembrane helix VI plays a role in activation of various G-protein-coupled receptors. Here we show that a mutation in this domain of the beta(2)-adrenergic receptor abolishes agonist activation...

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