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PMID: 2174879 Published · ppublish English Comparative Study Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S.

An aspartate conserved among G-protein receptors confers allosteric regulation of alpha 2-adrenergic receptors by sodium.

The Journal of biological chemistry ·Vol. 265 ·No. 35 ·1990-12-15 ·Pages 21590-5

Horstman DA, Brandon S, Wilson AL, Guyer CA, Cragoe EJ, Limbird LE

Abstract

The residue involved in sodium regulation of G-protein-coupled receptors has been identified by site-directed mutagenesis of the alpha 2-adrenergic receptor gene. Mutation of Asp-79 to Asn-79 entirely eliminates allosteric regulation of ligand binding by monovalent cations without perturbing the selectivity of adrenergic binding or allosteric modulation of that binding by amiloride analogs. The high degree of conservation of this aspartate residue in all G-protein-coupled receptors, without even a conservative change to glutamate, underscores the probable importance of this allosteric regulation.

MeSH Terms
Affinity Labels Allosteric Regulation Amino Acid Sequence Animals Aspartic Acid/physiology Brimonidine Tartrate DNA Mutational Analysis Dioxanes/metabolism Epinephrine/metabolism Idazoxan In Vitro Techniques Molecular Sequence Data Oxymetazoline/metabolism Prazosin/metabolism Quinoxalines/metabolism Receptors, Adrenergic, alpha/physiology Sodium/physiology Structure-Activity Relationship Swine Transfection Yohimbine/metabolism
Chemicals
Affinity Labels Dioxanes Quinoxalines Receptors, Adrenergic, alpha Yohimbine Aspartic Acid Brimonidine Tartrate Oxymetazoline Sodium Prazosin Idazoxan Epinephrine
Authors & Affiliations
6 authors, click to expand affiliations / ORCID
Horstman D A
Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-6600.
Brandon S
Wilson A L
Guyer C A
Cragoe E J
Limbird L E
Article Info
Journal
The Journal of biological chemistry
Abbr.
J Biol Chem
ISSN
0021-9258
Published
1990-12-15
Pages
21590-5
Language
English
Region
United States
NLM ID
2985121R
Subset
IM
Grants
NIGMS NIH HHS · GM07628 · United States
NHLBI NIH HHS · HL25182 · United States
NHLBI NIH HHS · HL43671 · United States
External Links
PubMed source View journal details
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