Affiliation:
1. Department of Medicine, Duke University Medical Center, Durham, North Carolina 27710.
Abstract
Adrenergic receptors are prototypic models for the study of the relations between structure and function of G protein-coupled receptors. Each receptor is encoded by a distinct gene. These receptors are integral membrane proteins with several striking structural features. They consist of a single subunit containing seven stretches of 20-28 hydrophobic amino acids that represent potential membrane-spanning alpha-helixes. Many of these receptors share considerable amino acid sequence homology, particularly in the transmembrane domains. All of these macromolecules share other similarities that include one or more potential sites of extracellular N-linked glycosylation near the amino terminus and several potential sites of regulatory phosphorylation that are located intracellularly. By using a variety of techniques, it has been demonstrated that various regions of the receptor molecules are critical for different receptor functions. The seven transmembrane regions of the receptors appear to form a ligand-binding pocket. Cysteine residues in the extracellular domains may stabilize the ligand-binding pocket by participating in disulfide bonds. The cytoplasmic domains contain regions capable of interacting with G proteins and various kinases and are therefore important in such processes as signal transduction, receptor-G protein coupling, receptor sequestration, and down-regulation. Finally, regions of these macromolecules may undergo posttranslational modifications important in the regulation of receptor function. Our understanding of these complex relations is constantly evolving and much work remains to be done. Greater understanding of the basic mechanisms involved in G protein-coupled, receptor-mediated signal transduction may provide leads into the nature of certain pathophysiological states.
Publisher
Ovid Technologies (Wolters Kluwer Health)
Reference120 articles.
1. Reis DJ Morrison S Ruggiero DA: The Cl area of the brainstem in tonic and reflex control of blood pressure. Hypertension 1988;ll(suppl I):I-8-I-13
2. van Zwieten PA Jie K van Brummelen P: Postsynaptic a r and a^-adrenoceptor changes in hypertension. / Cardiovasc Pharmacol 1987;10(suppl 4):568-575
3. Brodde O-E: Cardiac beta-adrenergic receptors. ISI Atlas of Scv Pharmacol 1987;l:107-112
4. Ruffolo AR Jr Nichols AJ Hieble JP: Functions mediated by alpha-2 adrenergic receptors in Limbird LE (ed): TheAlpha-2 Adrenergic Receptors. Clifton NJ Humana 1988 pp 187-280
5. Bernard C: Lecons Sur Us Proprietes Physiologique des Liquides de 1'Organisme. Paris Bailliere 1859 pp 172-173
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