PMID: 9658585Jul 11, 1998Paper

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

Il Farmaco
Susanna CotecchiaP G De Benedetti

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.

References

Oct 1, 1992·Trends in Pharmacological Sciences·W Schütz, M Freissmuth
Apr 1, 1990·Proceedings of the National Academy of Sciences of the United States of America·S CotecchiaR J Lefkowitz
Oct 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·S CotecchiaB K Kobilka
Jul 1, 1987·Proceedings of the National Academy of Sciences of the United States of America·C D StraderR A Dixon
Jan 1, 1995·Trends in Pharmacological Sciences·G MilliganM Lee
Aug 1, 1993·Trends in Pharmacological Sciences·R J LefkowitzT Costa
Feb 4, 1997·Proceedings of the National Academy of Sciences of the United States of America·A ScheerS Cotecchia
Oct 23, 1997·Proceedings of the National Academy of Sciences of the United States of America·A CavalliS Cotecchia

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