A Single Amino Acid Substitution in the β-Adrenergic Receptor Promotes Partial Agonist Activity from Antagonists

The family of G-protein-linked receptors includes many important pharmacological targets, of which the β-adrenergic receptor is one of the best characterized. A better understanding of those factors that determine whether a ligand functions as an antagonist or as an agonist would facilitate the deve...

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Veröffentlicht in:	The Journal of biological chemistry 1989-10, Vol.264 (28), p.16470-16477
Hauptverfasser:	Strader, C D, Candelore, M R, Hill, W S, Dixon, R A F, Sigal, I S
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenylyl Cyclase Inhibitors Adenylyl Cyclases - metabolism Adrenergic beta-Agonists - pharmacology Adrenergic beta-Antagonists - pharmacology Animals Aspartic Acid Biological and medical sciences Cell Membrane - metabolism Cell receptors Cell structures and functions Cricetinae Fundamental and applied biological sciences. Psychology Genes Glutamates Glutamic Acid Kinetics L Cells - metabolism Mice Models, Molecular Molecular and cellular biology Molecular Conformation Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine) Mutation Receptors, Adrenergic, beta - drug effects Receptors, Adrenergic, beta - genetics Receptors, Adrenergic, beta - metabolism Structure-Activity Relationship Transfection
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