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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
