title: Nature and uses of fluorescent dyes for drug transporter studies.
abstract: BACKGROUND
  Drug transporters are now recognized as major players involved in pharmacokinetics and toxicology. Methods for assessing their activity are important to consider, particularly owing to regulatory requirements with respect to inhibition of drug transporter activity and prediction of drug-drug interactions. In this context, the use of fluorescent-dye-based transport assays is likely to deserve attention.
  
  
  METHODS
  This review provides an overview of the nature of fluorescent dye substrates for ATP-binding cassette and solute carrier drug transporters. Their use for investigating drug transporter activity in cultured cells and clinical hematological samples, drug transporter inhibition, drug transporter imaging and drug transport at the organ level are summarized.
  
  
  CONCLUSIONS
  A wide range of fluorescent dyes is now available for use in various aspects of drug transporter studies. The use of these dyes for transporter analyses may, however, be hampered by classic pitfalls of fluorescence technology, such as quenching. Transporter-independent processes such as passive diffusion of dyes through plasma membrane or dye sequestration into subcellular compartments must also be considered, as well as the redundant handling by various distinct transporters of some fluorescent probes. Finally, standardization of dye-based transport assays remains an important on-going issue.
authors.affiliation: Institut de Recherches en Santé, Environnement et Travail (IRSET) , UMR INSERM U1085, Faculté de Pharmacie, 2 Avenue du Pr Léon Bernard, 35043 Rennes , France olivier.fardel@univ-rennes1.fr.
authors.forename: Olivier
authors.initials: O
authors.lastname: Fardel
authors.forename: Marc
authors.initials: M
authors.lastname: Le Vee
authors.forename: Elodie
authors.initials: E
authors.lastname: Jouan
authors.forename: Claire
authors.initials: C
authors.lastname: Denizot
authors.forename: Yannick
authors.initials: Y
authors.lastname: Parmentier
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D000818:Animals; D001692:Biological Transport; D002462:Cell Membrane / Q000378:metabolism; D004347:Drug Interactions; D005456:Fluorescent Dyes / Q000493:pharmacokinetics*; D006801:Humans; D026901:Membrane Transport Proteins / Q000378:metabolism*
chemical_list: D018528:ATP-Binding Cassette Transporters; D005456:Fluorescent Dyes; D026901:Membrane Transport Proteins
keywords: drug transporters; drug–drug interactions; fluorescent dyes; high-throughput assays; imaging; inhibitors