title: Receptor-drug interaction: europium employment for studying the biochemical pathway of g-protein-coupled receptor activation.
abstract: In medicinal chemistry field, the biochemical pathways, involved in 7-transmembrane domains G-protein coupled receptors (GPCRs) activation, are commonly studied to establish the activity of ligands towards GPCRs. The most studied steps are the measurement of activated GTP-alpha subunit and stimulated intracellular cAMP. At the present, many researchers defined agonist or antagonist activity of potential GPCRs drugs employing [(35)S]GTPgammaS or [(3)H]cAMP as probes. Recently, the corresponding lanthanide labels Eu-GTP and Eu-cAMP as alternative to radiochemicals have been developed because they are highly sensitive, easy to automate, easily synthesized, they display a much longer shelf-life and they can be used in multilabel experiments. In the present review, the receptor-drug interaction by europium employment for studying the biochemical pathway of GPCR activation has been focused. Moreover, comparative studies between lanthanide label probes and the corresponding radiolabeled compounds have been carried out.
authors: Dipartimento Farmacochimico, Facoltá di Farmacia, Universitá degli Studi di Bari, via Orabona 4, 70125 Bari, Italy.
authors: Colabufo Nicola
authors: CN
authors: Antonio
authors: Perrone Maria
authors: PM
authors: Grazia
authors: Contino
authors: C
authors: Marialessandra
authors: Berardi
authors: B
authors: Francesco
authors: Perrone
authors: P
authors: Roberto