Fig. 5: PSFL77, a newly discovered P2X3 enhancer, may exert its effects at a specific site within ICD of P2X3 receptors. | Nature Communications

Fig. 5: PSFL77, a newly discovered P2X3 enhancer, may exert its effects at a specific site within ICD of P2X3 receptors.

From: Finely ordered intracellular ___domain harbors an allosteric site to modulate physiopathological function of P2X3 receptors

Fig. 5

A Chemical structure of PSFL77. B Concentration-response curves showing effects of PSFL77 on the current amplitude of P2X3 induced by 0.1 μM or 10 μM ATP. The y axis signifies the normalized fold of current increase, calculated as the ratio of the current observed with PSFL77 to that recorded without PSFL77. Data are expressed as mean ± S.E.M. n = 6 (1, 3 and 10 μM), or 5 (30 and 100 μM) independent cells for 10 μM ATP, n = 4 (1, 3, 10, 30 and 100 μM) independent cells for 0.1 μM ATP. C Concentration-response curves employed to illustrate the influence of PSFL77 on the desensitization of P2X3 receptors at 0.1 μM or 10 μM ATP. The y axis shows the altered normalized ratio, calculated by dividing the current at 1 s after reaching the maximum by the maximum current amplitude. Data are expressed as mean ± S.E.M. n = 6 (1, 3 and 10 μM), or 5 (30 and 100 μM) independent cells for 10 μM ATP, n = 4 (1, 3, 10, 30 and 100 μM) independent cells for 0.1 μM ATP. D Pooled data showing the effects of PSFL77 (100 μM) on P2X3, P2X1, P2X2, P2X4 and P2X7 receptors. The y axis indicates the fold increase in current induced by PSFL77, with each open circle representing an individual measurement (mean ± S.E.M., n = 5 (P2X1, P2X2, P2X4 and P2X7) or 8 (P2X3). E Application of PSFL77 (100 μM) via patch pipettes on rP2X3 receptors. Consistent traces across three repetitions were obtained. F Schematic diagram illustrates the strategy employed for constructing chimeras of rP2X2 and rP2X3. G, H Representative current traces (G) and summarized data (H) to show the effect of PSFL77 (100 μM) on ATP (10 μM)-induced activation of the rP2X2/rP2X3 chimeras. The scatter of each open circle represents an individual measurement (mean ± S.E.M., n = 5 (rP2X2WT and CH2), 7 (CH2) or 8(rP2X3WT)), **P < 0.01 vs. rP2X3WT; #P < 0.05 vs. rP2X2WT, one-way ANOVA with Dunnett’s multiple comparisons test, P = 0.0050 (rP2X2WT vs. rP2X3WT), 0.0044 (CH1 vs. rP2X3WT), and 0.0016 (CH2 vs. rP2X2WT). Data from WT P2X3 in D were replotted in H for comparison. I Concentration-response curve of PSFL77 on the current amplitude of the chimera CH2 activated by 10 μM ATP. The y axis shows the normalized current increase, derived from the ratio of ATP- current with and without PSFL77. Data are expressed as mean ± S.E.M. n = 4 (1, 3, 10, 30 and 100 μM) independent cells for CH2.

Back to article page