IndraLab

Statements

ML335 activates KCNK2. 3 / 3
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"We then started a three-day intra-tracheal treatment course with the novel TREK-1 activating compounds BL1249 or ML335."
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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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