Genetic Analysis of the β-Adrenergic Receptor
Many hormone and neurotransmitter receptors mediate their signals through interaction with guanine nucleotide-binding regulatory proteins (G-proteins) (see Gilman, 1987, for review). As described elsewhere in this volume, the cloning of the genes for these receptor proteins has revealed a large degree of structural homology within this family of receptors. The homology among the receptors is concentrated within the hydrophobic cores of the proteins, formed by the seven putative transmembrane helices, whereas the extracellular and intracellular hydrophilic loop regions are more divergent. Although the hormones and neurotransmitters which couple various receptors to G-protein-mediated signaling pathways represent a diverse group of small molecule and peptide ligands, there are striking parallels in their mechanisms of signal transduction. Thus, the structural similarities among G-protein-coupled receptors probably reflect similar molecular interactions which are responsible for their common mechanism of action. For this reason, the structural and functional information obtained for one of these receptor proteins should be applicable to the entire family of G-protein-coupled receptors.
KeywordsLigand Binding Site Mutant Receptor Muscarinic Acetylcholine Receptor Chimeric Receptor Antagonist Binding
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