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.

Molecular mechanisms involved in the activation and regulation of the alpha 1-adrenergic receptor subtypes / S., Cotecchia; A., Scheer; D., Diviani; Fanelli, Francesca; DE BENEDETTI, Pier Giuseppe. - In: IL FARMACO. - ISSN 0014-827X. - ELETTRONICO. - 53:(1998), pp. 273-277. [10.1016/S0014-827X(98)00021-4]

Molecular mechanisms involved in the activation and regulation of the alpha 1-adrenergic receptor subtypes

FANELLI, Francesca;DE BENEDETTI, Pier Giuseppe
1998

Abstract

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.
53
273
277
Molecular mechanisms involved in the activation and regulation of the alpha 1-adrenergic receptor subtypes / S., Cotecchia; A., Scheer; D., Diviani; Fanelli, Francesca; DE BENEDETTI, Pier Giuseppe. - In: IL FARMACO. - ISSN 0014-827X. - ELETTRONICO. - 53:(1998), pp. 273-277. [10.1016/S0014-827X(98)00021-4]
S., Cotecchia; A., Scheer; D., Diviani; Fanelli, Francesca; DE BENEDETTI, Pier Giuseppe
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/310539
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