Figure 6.
Critical binding sites for gating modifiers IAA and IAB in mouse TRPV3 channel. Representative bound conformations of IAA (A) and IAB (B) confined to the pocket consisting of the pore helix and S6 segment in top-down view (left panel) and side view (right panel). IAA and IAB are shown in red and purple surfaces, respectively. Side view of IAA (green) and TRPV3 subunit interactions (C), and IAB (green) and TRPV3 subunit interactions (D). Hydrogen bonds and van der Waals forces are shown as orange and light blue dotted lines, respectively. Three TRPV3 subunits are shown in blue, cyan and yellow. Representative current traces of wild type mTRPV3 (E and F), T636A (G) and F666A (H) mutants expressed in HEK293 cells in responses to 2-APB alone and 2-APB with IAA or IAB. (I) Summary for WT mTRPV3 or mutant channel current inhibition by 50 μmol/L IAA and IAB (n = 3–8). Data are shown as the mean ± SEM, ∗∗∗P < 0.001, by unpaired t test.