Adrenergic receptors. Models for regulation of signal transduction processes.
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.
Type
Journal articleSubject
Amino Acid SequenceGTP-Binding Proteins
Molecular Sequence Data
Receptors, Adrenergic
Signal Transduction
Structure-Activity Relationship
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Marc G. Caron
James B. Duke Distinguished Professor of Cell Biology
Studies of the mechanisms of action and regulation of hormones and neurotransmitters
at the cellular and molecular levels constitute the main goals our of research activities.
G protein-coupled receptors (GPCR) mediate the actions of signaling molecules from
unicellular organisms to man. We have used adrenergic and dopamine receptors to characterize
the structure/function and regulation mechanisms of these prototypes of G protein-coupled
receptors. Another approach has been to characterize
This author no longer has a Scholars@Duke profile, so the information shown here reflects
their Duke status at the time this item was deposited.
Robert J. Lefkowitz
The Chancellor's Distinguished Professor of Medicine
Dr. Lefkowitz’s memoir, A Funny Thing Happened on the Way to Stockholm, recounts his
early career as a cardiologist and his transition to biochemistry, which led to his
Nobel Prize win.
Robert J. Lefkowitz, M.D. is Chancellor’s Distinguished Professor of Medicine and
Professor of Biochemistry and Chemistry at the Duke University Medical Center. He
has bee
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