Fig. 8: PSFL2915 blocks the conformational changes of IP-HD in P2X3 induced by ATP binding.
From: Chronic cough relief by allosteric modulation of P2X3 without taste disturbance
a Effect of PSFL2915 (1 μM) on ATP (1, 10, 100 μM)-induced activation of WT hP2X3. Each circle represents an independent cell. n = 5 (1 μM) or 6 (10 and 100 μM); one-way ANOVA and Dunnett’s multiple comparison test, F (2, 14) = 0.8142. Data are expressed as mean ± SEM. b DTNB (2 mM) modification reduced the inhibition of hP2X3S67C by PSFL2915 (1 μM). Each line represents an independent cell, n = 5. P value was calculated from a paired, two-tailed t test. c Effect of PSFL2915 (1 μM) on ATP (100 μM) induced activation of hP2X4 and hP2X4P2X3 (C107-C153). Each circle represents an independent cell; n = 3. P value was calculated from an unpaired, two-tailed t test. Data are expressed as mean ± SEM. d, e Representative emission spectra in the absence and presence of ATP (10 µM) for WT hP2X3. f Zoomed-in view of the location of L297 and bound quercetin. g DTNB (2 mM) modification did not reduce the inhibition rate of hP2X3L297C by quercetin (10 μM). Each line represents an independent cell, n = 3; paired two-tailed t test. h, i Representative emission spectra in the absence and presence of ATP (10 µM) for the ATP-induced shift of the peak emission wavelengths for hP2X3L297ANAP. d, e, h, i PSFL2915 (500 nM) was applied as indicated. Black, control; red, emission spectrum in the presence of 10 μM ATP; dark cyan, emission spectra in the presence of 10 μM ATP and 500 nM PSFL2915. j Pooled data for experiments in d, e, h, i. Each line represents an independent cell; n = 5. P value was calculated from a paired, two-tailed t test. Source data are provided as a Source Data file.
