Fig. 7: Kv7.3-W265 is required for gentisic acid opening of Kv7.2/3. | Communications Chemistry

Fig. 7: Kv7.3-W265 is required for gentisic acid opening of Kv7.2/3.

From: Discovery of a potent, Kv7.3-selective potassium channel opener from a Polynesian traditional botanical anticonvulsant

Fig. 7

a Electrostatic surface potential (left; red = negative, blue = positive) and structure (right; red = oxygen, blue = nitrogen) for portia tree compounds tested herein. b Unbiased SwissDock predicted binding of gentisic acid (blue; multiple binding poses indicated) to Kv7.3-W265 (seafoam green). Kv7.3 transmembrane segments (Sx) and pore (P) labeled). c Close-up of one gentisic binding pose from panel (b), with wireframe surface plots shown. d Mean traces for Kv7.2/3 mutant combinations as indicated, expressed in oocytes in the absence (Control) or presence of gentisic acid (100 µM). Scale bars lower left; voltage protocol center inset; n = 9 (Kv7.2/Kv7.3-W265L), 5 (Kv7.2-W236L/Kv7.2), 8 (Kv7.2L-W236L/Kv7.3-W265L). e Mean raw tail current/voltage relationship (left) and normalized tail current (G/Gmax)/voltage relationship (right) for traces as in (d); n values as in (d). f Mean unclamped oocyte membrane potential for mutant Kv7.2/3-expressing oocytes as in (d); n values as in (d). Error bars indicate SEM. n indicates number of biologically independent oocytes. Statistical comparisons by t-test.

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