[35S]GTPγS binding studies of amphiphilic drugs-activated Gi proteins: A caveat |
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Authors: | Dina Manetti Lorenzo Di Cesare Mannelli Silvia Dei Luca Guandalini Elisabetta Martini Martina Banchelli Carla Ghelardini |
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Institution: | 1. Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente Attivi (HeteroBioLab), Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via U. Schiff 6, 50019 Sesto Fiorentino (FI), Italy;2. Dipartimento di Farmacologia Preclinica e Clinica, Università di Firenze, Viale G. Pieraccini 6, 50139 Firenze, Italy;3. Dipartimento di Chimica e CSGI, Università di Firenze, Via della Lastruccia 3, 50019 Sesto Fiorentino (FI), Italy |
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Abstract: | This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of 35S]GTPγS to different subtypes of Gi protein. The problem arose from the strong affinity between 35S]GTPγS and the tested compounds, that are characterized by several (2–4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results. |
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