title: Bright, highly water-soluble triazacyclononane europium complexes to detect ligand binding with time-resolved FRET microscopy.
abstract: Luminescent europium complexes are used in a broad range of applications as a result of their particular emissive properties. The synthesis and application of bright, highly water-soluble, and negatively charged sulfonic- or carboxylic acid derivatives of para-substituted aryl-alkynyl triazacyclononane complexes are described. Introduction of the charged solubilizing moieties suppresses cellular uptake or adsorption to living cells making them applicable for labeling and performing assays on membrane receptors. These europium complexes are applied to monitor fluorescent ligand binding on cell-surface proteins with time-resolved Förster resonance energy transfer (TR-FRET) assays in plate-based format and using TR-FRET microscopy.
authors.affiliation: Department of Chemistry, Durham University, South Road, DH1 3LE, Durham (UK).
authors.forename: Martina
authors.initials: M
authors.lastname: Delbianco
authors.forename: Victoria
authors.initials: V
authors.lastname: Sadovnikova
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Bourrier
authors.forename: Gérard
authors.initials: G
authors.lastname: Mathis
authors.forename: Laurent
authors.initials: L
authors.lastname: Lamarque
authors.forename: Jurriaan M
authors.initials: JM
authors.lastname: Zwier
authors.forename: David
authors.initials: D
authors.lastname: Parker
mesh_terms: D001372:Aza Compounds / Q000032:analysis* / Q000378:metabolism; D056831:Coordination Complexes / Q000032:analysis* / Q000378:metabolism; D005063:Europium / Q000032:analysis* / Q000378:metabolism; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D057809:HEK293 Cells; D006801:Humans; D008024:Ligands; D049408:Luminescent Agents / Q000032:analysis* / Q000378:metabolism; D008853:Microscopy / Q000379:methods*; D010880:Piperidines / Q000032:analysis* / Q000378:metabolism; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000032:analysis / Q000378:metabolism*; D012995:Solubility; D014867:Water / Q000737:chemistry
chemical_list: D001372:Aza Compounds; D056831:Coordination Complexes; D008024:Ligands; D049408:Luminescent Agents; D010880:Piperidines; D043562:Receptors, G-Protein-Coupled; C482777:triazacyclononane; D014867:Water; D005063:Europium
keywords: G protein-coupled receptors; europium; imaging agents; macrocycles; time-resolved FRET