IndraLab

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ML402 activates KCNK2. 5 / 5
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"Because K modulator pocket contains architectural elements that support the selectivity and GOF mutant sites that activate the C-type gate , we asked whether P1/M4 interface structural changes caused by ML335, ML402, or GOF mutation impact C-type gate function.Measurement of K 2.1(TREK-1) in inside-out patches under conditions that potentiate flux-dependent C-type gate activation (150 mM K versus 150 mM Rb ) showed the expected outward rectification (Fig. 4g and k)."
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"ML335 and ML402 are remarkably selective, activating K 2.1 (TREK-1) and K 10.1 (TREK-2) but not K 4.1 (TRAAK) [11] (Fig. 4.3)."
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"The L2/L3 site seems to be a prime point for modulatory lipids, as the positively charged residues that affect PIP responses are on the helical face opposite to L2/L3 and M4 conformational changes could affect how these residues interact with regulatory lipid headgroups.Xenopus oocyte two electrode voltage-clamp measurements show that ML335 and ML402 activate K 2.1(TREK-1) and K 10.1(TREK-2) but not K 4.1(TRAAK) (14.3 ± 2.7 μM, K 2.1(TREK-1):ML335; 13.7± 7.0 μM, K 2.1(TREK-1):ML402; 5.2 ± 0.5 μM, K 10.1(TREK-2):ML335; and 5.9 ± 1.6 μM, K 10.1(TREK-2):ML402) (Fig. 4a–f, Extended Data Fig. 7a–c)."
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"Xenopus oocyte two electrode voltage-clamp measurements show that ML335 and ML402 activate K 2.1(TREK-1) and K 10.1(TREK-2) but not K 4.1(TRAAK) (14.3 ± 2.7 μM, K 2.1(TREK-1):ML335; 13.7± 7.0 μM, K 2.1(TREK-1):ML402; 5.2 ± 0.5 μM, K 10.1(TREK-2):ML335; and 5.9 ± 1.6 μM, K 10.1(TREK-2):ML402) (Fig. 4a–f, Extended Data Fig. 7a–c)."
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"ML335 and ML402 activate K 2.1(TREK-1) in HEK293 cells similar to their effects in Xenopus oocytes (5.2 ± 0.8 μM and 5.9 ± 1.6 μM for ML335 and ML402, respectively (n≥3)) (Fig. 4g–i, Extended Data Fig. 8a)."
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