Molecular mechanisms involved in the activation and regulation of the alpha 1-adrenergic receptor subtypes.
The adrenergic receptors (ARs) belong to the superfamily of membrane-bound G protein coupled receptors (GPCRs). Our investigation has focused on the structure-function relationship of the alpha 1b-AR subtype used as the model system for other GPCRs. Site-directed mutagenesis studies have elucidated the structural domains of the alpha 1b-AR involved in ligand binding, G protein coupling or desensitization. In addition, a combined approach using site-directed mutagenesis and molecular dynamics analysis of the alpha 1b-AR has provided information about the potential mechanisms underlying the activation process of the receptor, i.e. its transition from the 'inactive' to the 'active' conformation.
Cotecchia
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S
Institut de Pharmacologie et Toxicologie, Faculté de Médecine, Lausanne, Switzerland. susanna.cotecchia@ipharm.unil.ch
Scheer
A
A
Diviani
D
D
Fanelli
F
F
De Benedetti
P G
PG
D000595:Amino Acid Sequence; D000818:Animals; D019204:GTP-Binding Proteins / Q000502:physiology; D006801:Humans; D008969:Molecular Sequence Data; D016297:Mutagenesis, Site-Directed; D018340:Receptors, Adrenergic, alpha-1 / Q000737:chemistry / Q000145:classification*; D013329:Structure-Activity Relationship
D018340:Receptors, Adrenergic, alpha-1; D019204:GTP-Binding Proteins