ArticleBioorganic & medicinal chemistry2009
Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines.
Article in Bioorganic & medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
6 citing papers in PubMed.
- Ligands of Adrenergic Receptors: A Structural Point of View.Biomolecules · 2021Review
- Influence of Fluorination on the Conformational Properties and Hydrogen-Bond Acidity of Benzyl Alcohol Derivatives.Chemistry (Weinheim an der Bergstrasse, Germany) · 2015Article
- Graph analysis of β2 adrenergic receptor structures: a "social network" of GPCR residues.In silico pharmacology · 2013Article
- Comparison of dynamics of extracellular accesses to the β(1) and β(2) adrenoceptors binding sites uncovers the potential of kinetic basis of antagonist selectivity.Chemical biology & drug design · 2012Article
- GPCR agonist binding revealed by modeling and crystallography.Trends in pharmacological sciences · 2011Article
- Progress in structure based drug design for G protein-coupled receptors.Journal of medicinal chemistry · 2011Review
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
The important and diverse biological functions of adrenergic receptors, a subclass of G protein-coupled receptors (GPCRs), have made the search for compounds that selectively stimulate or inhibit the activity of different adrenergic receptor subtypes an important area of medicinal chemistry. We previously synthesized 2-, 5-, and 6-fluoronorepinehprine (FNE) and 2-, 5-, and 6-fluoroepinephrine (FEPI) and found that 2FNE and 2FEPI were selective beta-adrenergic agonists and that 6FNE and 6FEPI were selective alpha-adrenergic agonists, while 5FNE and 5FEPI were unselective. Agonist potencies correlated well with receptor binding affinities. Here, through a combination of molecular modeling and site-directed mutagenesis, we have identified N293 in the beta(2)-adrenergic receptor as a crucial residue for the selectivity of the receptor for catecholamines fluorinated at different positions.
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Registered trials
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