title: Fluorescent ligands for adenosine receptors.
abstract: Interest is increasing in developing fluorescent ligands for characterization of adenosine receptors (ARs), which hold a promise of usefulness in the drug discovery process. The size of a strategically labeled AR ligand can be greatly increased after the attachment of a fluorophore. The choice of dye moiety (e.g. Alexa Fluor 488), attachment point and linker length can alter the selectivity and potency of the parent molecule. Fluorescent derivatives of adenosine agonists and antagonists (e.g. XAC and other heterocyclic antagonist scaffolds) have been synthesized and characterized pharmacologically. Some are useful AR probes for flow cytometry, fluorescence correlation spectroscopy, fluorescence microscopy, fluorescence polarization, fluorescence resonance energy transfer, and scanning confocal microscopy. Thus, the approach of fluorescent labeled GPCR ligands, including those for ARs, is a growing dynamic research field.
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA.
authors.forename: Eszter
authors.initials: E
authors.lastname: Kozma
authors.forename: P Suresh
authors.initials: PS
authors.lastname: Jayasekara
authors.forename: Lucia
authors.initials: L
authors.lastname: Squarcialupi
authors.forename: Silvia
authors.initials: S
authors.lastname: Paoletta
authors.forename: Stefano
authors.initials: S
authors.lastname: Moro
authors.forename: Stephanie
authors.initials: S
authors.lastname: Federico
authors.forename: Giampiero
authors.initials: G
authors.lastname: Spalluto
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Jacobson
mesh_terms: D001896:Boron Compounds / Q000737:chemistry; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D058906:Purinergic P1 Receptor Agonists / Q000737:chemistry / Q000378:metabolism; D058915:Purinergic P1 Receptor Antagonists / Q000737:chemistry / Q000378:metabolism; D018047:Receptors, Purinergic P1 / Q000737:chemistry* / Q000378:metabolism
chemical_list: C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D005456:Fluorescent Dyes; D008024:Ligands; D058906:Purinergic P1 Receptor Agonists; D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1; D016650:Fluorescein-5-isothiocyanate