Since biological assays are essential in the early development of new drugs, there is increasing request of easy, robust, and not radioactive assays. GTP-Eu binding assay is a new no-radioactive tool produced by Perkin-Elmer company to screen compounds active at G-protein-coupled receptors [1]. This methodology can be considered a valid and powerful alternative to the well-known [35S]GTPγS binding assay, and it is based on the time-resolved fluorometry technique that exploits the fluorescence properties of lanthanide chelate europium. The aim of this work was the application and optimization of this procedure at adenosine A3 Gαi-coupled receptor in order to test new ligand activity with an assay endowed with high sensitivity, long shelf life, amenability to automation, and safety.

GTP-Eu binding assay optimization for the adenosine A3 receptor ligands screening

BUCCIONI, Michela;DAL BEN, DIEGO;MARUCCI, Gabriella;VOLPINI, Rosaria;CRISTALLI, Gloria
2010-01-01

Abstract

Since biological assays are essential in the early development of new drugs, there is increasing request of easy, robust, and not radioactive assays. GTP-Eu binding assay is a new no-radioactive tool produced by Perkin-Elmer company to screen compounds active at G-protein-coupled receptors [1]. This methodology can be considered a valid and powerful alternative to the well-known [35S]GTPγS binding assay, and it is based on the time-resolved fluorometry technique that exploits the fluorescence properties of lanthanide chelate europium. The aim of this work was the application and optimization of this procedure at adenosine A3 Gαi-coupled receptor in order to test new ligand activity with an assay endowed with high sensitivity, long shelf life, amenability to automation, and safety.
2010
274
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11581/250536
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