title: Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.
abstract: The use of G protein-coupled receptors fluorescent ligands is undergoing continuous expansion. In line with this, fluorescent agonists and antagonists of high affinity for G protein-coupled adenosine and P2Y receptors have been shown to be useful pharmacological probe compounds. Fluorescent ligands for A1R, A2AR, and A3R (adenosine receptors) and P2Y2R, P2Y4R, P2Y6R, and P2Y14R (nucleotide receptors) have been reported. Such ligands have been successfully applied to drug discovery and to GPCR characterization by flow cytometry, fluorescence correlation spectroscopy, fluorescence microscopy, fluorescence polarization, fluorescence resonance energy transfer and scanning confocal microscopy. Here we summarize recently reported and readily available representative fluorescent ligands of purinergic receptors. In addition, we pay special attention on the use of this family of fluorescent ligands revealing two main aspects of purinergic receptor biology, namely ligand binding and receptor oligomerization. This article is part of the Special Issue entitled 'Fluorescent Tools in Neuropharmacology'.
authors.affiliation: Unitat de Farmacologia, Departament Patologia i Terapèutica Experimental, Facultat de Medicina, IDIBELL, Universitat de Barcelona, 08907 L'Hospitalet de Llobregat, Spain; Department of Physiology, Faculty of Sciences, University of Ghent, 9000 Gent, Belgium. Electronic address: fciruela@ub.edu.
authors.forename: Francisco
authors.initials: F
authors.lastname: Ciruela
authors.affiliation: Unitat de Farmacologia, Departament Patologia i Terapèutica Experimental, Facultat de Medicina, IDIBELL, Universitat de Barcelona, 08907 L'Hospitalet de Llobregat, Spain.
authors.forename: Víctor
authors.initials: V
authors.lastname: Fernández-Dueñas
authors.affiliation: Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, 20892 Bethesda, USA. Electronic address: kajacobs@helix.nih.gov.
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Jacobson
mesh_terms: D000818:Animals; D057005:Bioengineering; D005456:Fluorescent Dyes / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D008027:Light; D008856:Microscopy, Fluorescence; D011485:Protein Binding / Q000187:drug effects; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
chemical_list: D005456:Fluorescent Dyes; D043562:Receptors, G-Protein-Coupled
keywords: FRET; Fluorescent ligands; GPCR oligomerization; Purinergic receptors