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. 2014 Apr 30;9(7):1420–1425. doi: 10.1021/cb500063y

Figure 3.

Figure 3

(a) Competition binding assays of [Y]6-AII analogue to AT1R, AT2R wild type, and mutants: AT1R, open circle; wild type AT2R, black circles; AT2R-Y189A, blue diamonds; AT2R-Y189N, green triangle; AT2R-F272(6.51)A, red square; AT2R-F272(6.51)H, orange triangle. Kd and Ki values are given in Supplementary Table S3. (b,c) Plots of fold selectivity values for the two AII receptor subtypes (IC50(AT1R)/IC50(AT2R)]) versus % of cis (b) and the value of Hammet substituent constants σpara (c) for the different AII analogues (see also Supplementary Table S5). (d) PC12W cells, either transduced with the Ad-AT2R or untransduced, were used for the evaluation of the AT2R agonistic effect of [Y]6-AII in the presence of either 1 nM AII or [Y]6-AII. Agonist-induced neurite outgrowth by AII or [Y]6-AII for 24 h stimulation was quantified by counting neurite-positive cell numbers in five randomly selected photos/well. The neurite outgrowth-positive cells were defined as the cells with neurite length longer than their cell diameters. This experiment was carried out in triplicate and repeated twice.