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P11012
Dual Purpose Cell Lines for Analysis of GPCR/Arrestin Interaction Using PathHunter & Natural Gq-coupling Using the Improved Calcium No-Wash PLUS Kit.
Presenter Tim Cloutier, DiscoveRx Corporation, USA
Additional Authors: Tom Wehrman, Chin-Yee Loh, Lakshmi Anantharaman, Neil Charter, and Keith R. Olson,Brenda Tierney

DiscoveRx has developed a panel of over 20 naturally Gq-coupled GPCR/Arrestin cell lines that can be used in screening and profiling applications for both arrestin biology and second messenger signaling. This presents a number of interesting use case scenarios, such as sequential monitoring of both readouts in a single screen, or use of the same cell line for analysis of both readouts at the hit ID and hit qualification stages. We will present data showing the validation of these cell lines with our new Calcium No-Wash PLUS Kit, and the comparison of the calcium results with the arrestin results for a number of test compounds. The results clearly show that the same cell line and the same receptor can show rather different pharmacology for the same set of targets, and in at least one case we can find a compound that shows clear arrestin bias and was not a hit in the calcium assay. We will also present data showing that we can in the same well and the same plate, first analyze the calcium response with our new kit, and follow that with analysis of the arrestin biology without the need for any media exchange.