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      Molecular Biology of Adrenergic Receptors: Model Systems for the Study of G-Protein-Mediated Signal Transduction


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          Elucidation of the gene structure of several receptors known to mediate the signal of hormone or transmitter binding to intracellular effector systems through guanine-nucleotide-binding proteins (G proteins) has revealed that these receptors comprise a super-family of related proteins. The hallmark of all G-protein-linked receptors is a presumed topography of 7 membrane-spanning loops, analogous to the structure of bacteriorhodopsin. Members of this gene superfamily contain regions, particularly with the hydrophobic domains, of homologous sequence. The expression of G-protein-linked receptors in heterologous cell systems has allowed for the study of the pharmacological and biochemical properties of individual receptor subtypes in a manner not previously possible with intact tissues containing multiple receptors. Site-directed mutagenesis experiments have identified many conserved amino acids which are involved in ligand binding, receptor activation by agonists and receptor-G protein coupling, and suggest that the conservation of receptor structure throughout this gene family may reflect a conservation of important functional domains within these proteins.

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          Author and article information

          J Vasc Res
          Journal of Vascular Research
          S. Karger AG
          23 September 2008
          : 28
          : 1-3
          : 93-103
          Section on Molecular Neurobiology, Laboratory of Physiologic and Pharmacologic Studies, National Institute on Alcohol Abuse and Alcoholism, Rockville, Md., USA
          158848 Blood Vessels 1991;28:93–103
          © 1991 S. Karger AG, Basel

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          Page count
          Pages: 11
          Signal Recognition and Transduction in Vascular Smooth Muscle

          General medicine,Neurology,Cardiovascular Medicine,Internal medicine,Nephrology
          Site-directed mutagenesis,Agonist activation,Signal transduction,G proteins,Amino acid homology,α-Adrenergic receptors,β-Adrenergic receptors,Muscarinic acetylcholine receptors,Ligand-binding site,Gene expression


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