Fig. 7: Applications and further investigations into basal activities revealed by Tango-Trio. | Nature Communications

Fig. 7: Applications and further investigations into basal activities revealed by Tango-Trio.

From: Profiling of basal and ligand-dependent GPCR activities by means of a polyvalent cell-based high-throughput platform

Fig. 7

HTTL-B1 and HTTL-B2 were transfected with GPCRs exhibiting strong basal arrestin recruitment. Transfected cells were stimulated as cumate dose-response in the presence or absence of the following inverse agonists/antagonists at saturating (EC80) concentrations: O-1918 at GPR55 (a, b), Cetirizine and Mepyramine at HRH1 (c, d), FC131 at CXCR4 (e, f), Tolvaptan at AVPR2 (g, h), Fluspirelene and Thioridazine at HTR1E (i, j), Pindolol, Alprenolol and Spiperone at HTR1B (k), Spiperone and Fluspirelene at HTR1D (l), and Clozapine, Thiothexene, Thioridazine and Fluspirelene at HTR5A (m). Dynamin-dependence of high basal internalization was tested by co-transfecting HTTL-F cells with GPR87 (n), CHRM5 (o), and HTR4 (p) with/without dynaminK44A. Transfected cells were stimulated as a cumate dose-response, and stimulation curves were built using XY analysis for non-linear regression curve and the 4-parameters dose-response stimulation function, followed by baseline correction. Data are presented as mean values, with error bars representing SEM. Data are representative of 2 biological replicates, with 3 technical replicates each. Generic receptor codes refer to the GPCR-Tango constructs.

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