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Table 2 Effect of mutations predicted by molecular modeling on the activation of the sweet taste receptor by neohesperidin dihydrochalcone (NHDC) and aspartame (ASP)

From: The binding site for neohesperidin dihydrochalcone at the human sweet taste receptor

variant NHDC EC50 (mM) NHDC maximal signal (% of wt) ASP EC50 (mM) ASP maximal signal (% of wt)
wt 0.1 ± 0.06 100 1.3 ± 0.1 100
S620A 2.57 1.3 ± 0.5 55 ± 80 1.2 ± 0.3 64 ± 4
V621L2.58 n.f. --- n.f. ---
V621I 2.58 >1 60 ± 14 1.9 ± 0.4 61 ± 1
F624L 2.61 >1 35 ± 70 1.4 ± 0.2 21 ± 4
Y699L 4.60 0.7 ± 0.1 83 ± 40 1.6 ± 0.4 78 ± 9
Y699F 4.60 0.6 ± 0.4 72 ± 17 1.2 ± 0.3 56 ± 2
T724L 5.37 0.5 ± 0.3 58 ± 60 1.5 ± 0.2 69 ± 2
R725M 5.38 1.3 ± 0.4 64 ± 14 1.5 ± 0.7 56 ± 1
S726A 5.39 0.9 ± 0.3 60 ± 50 0.9 ± 0.3 50 ± 2
L800F7.38 0.2 ± 0.1 91 ± 70 1.2 ± 0.3 90 ± 1
C801I 7.39 1.6 ± 0.7 70 ± 13 1.2 ± 0.5 50 ± 9
C801L7.39 n.f. --- n.f. ---
G804A 7.42 1.3 ± 0.5 53 ± 10 1.6 ± 0.2 44 ± 1
G804V 7.42 n.r. --- 1.3 ± 0.3 21 ± 2
  1. Receptor variants that affect the NHDC response are shown in bold. Values are given as average over at least three independent experiments ± SD. n.f. no response to any tested sweetener, n.r. no response to neohesperidin dihydrochalcone up to highest tested concentration (6 mM), but responses to other sweeteners. (>), EC50 not calculable because saturation is not reached (Additional file 2).