Fig. 1: LAKI selectively photo-controls TREK1, TREK2 and TRESK channels in a heterologous system.
From: A photoswitchable inhibitor of TREK channels controls pain in wild-type intact freely moving animals
a Design of LAKI from ML365 and photoisomerization of LAKI upon alternating illumination at 480 nm (blue) and 365 nm (magenta). b Normalized whole-cell current recording elicited at −60 mV from HEK293T cells expressing TREK1, TREK2, TRESK and TRAAK in the presence of LAKI (5 µM) upon alternating illumination at 480 nm (blue) and 365 nm (magenta). c Bar graph summarizing the current inhibition (%) of TREK1, TREK2, TRESK, TASK1, TASK3 and TRAAK at −60 mV. For each channel, n was obtained from one experiment. Statistical significance was determined by QuasiBinomial GLM followed by Dunnett’s post-test versus TASK1 (***p < 0.001). d Normalized whole-cell current recordings elicited at −60 mV from HEK293T cells expressing TRESK in the presence of several concentrations of LAKI upon alternating illumination at 480 nm (blue) and 365 nm (magenta). e Representative whole-cell current recording elicited at 0 mV from HEK293T expressing TRESK in the presence of LAKI (5 µM) upon illumination at 480 nm (blue) and 365 nm (magenta) or in the dark. f Whole-cell current recordings elicited at different holding potentials from HEK293T cells expressing TRESK in the presence of LAKI (5 µM) upon alternating illumination at 480 nm (blue) and 365 nm (magenta). g IV relationship of the photocurrent density induced by alternating illumination (I480 nm – I365 nm) at different holding potentials in HEK293T cells expressing TRESK in the presence of LAKI (5 µM). n was obtained from one experiment. Data were represented as mean ± SEM. The numbers of tested cells are indicated in parentheses on the graph.
