IndraLab

Statements



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"Insertion of PIP into the intracellular side of the membrane restores TREK1 activity."

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"Thus, we propose that PIP activates TREK-1 by promoting a transition from the down state to an up state that is capable of supporting a higher degree of channel activity."

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"PIP 2 can also indirectly activate TREK-1 through PIP 2 agonism of PLD2 [XREF_BIBR], making PIP 2 regulation complicated [XREF_BIBR]."

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"The potassium channel subfamily K member 2 (TREK-1) is both activated and inhibited by PIP 2 ."

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"In contrast with PG and PA, increasing concentrations of PIP 2 (0.5, 1, and 2 mol%) failed to activate TREK-1 : the highest concentration of PIP 2, 2 mol%, induced the least flux (XREF_FIG and XREF_FIG)."

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"Thus, they modeled the C-terminal domain into the down-state structure and investigated the binding and conformational modulation of TREK-1 by PIP 2 ."

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"As mentioned, PIP 2 could also indirectly activate TREK-1 through the enzyme PLD2."

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"Since TREK channels are activated by PIP 2 it is possible that the DCPIB effect is mediated via an allosteric enhancement of the PIP 2 effect rather than a direct competition with it."

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"These findings combined with Comoglio 's model of localization of PLD2 in the activation of TREK-1 suggest PIP 2 could indirectly activate TREK-1 through increasing PLD2 activation and production of PA and PG agonists (see XREF_SUPPLEMENTARY)."

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"Unexpectedly, sub-saturating PIP 2 (0.5 mol%) in the presence of 10 mol% PG enhanced TREK-1 activity (XREF_FIG and XREF_FIG)."