GPCR regulation through arrestin pathway using Nomad technology

Here we show a screening of compounds for Neurokinin 1 receptor regulation using Nomad technology through arrestin pathway. The Nomad biosensor localization is in the Plasma Membrane but the GPCR activation leads to a modification in its structural folding that promotes its vesicularization. In this work we have screened a library of 600 compounds. Substance P and L733-060 compounds were used as agonist and inhibitor control for this model. After the screening campaign, positive compounds were chosen for further testing, based on the strength of the initial response and the lack of cytotoxicity. Our results indicated that this model is a valid strategy for drug screening.