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Statements

KCNK2 binds phosphatidylinositol phosphate. 11 / 11
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"However, unlike the response observed with mPLD2, the association of TREK-1 with PIP 2 clusters remained relatively weak following shear forces ( xref ), despite an overall increase in TREK-1 and PIP 2 levels in the membrane prior to shear ( xref ). xref shows a model of shear-induced movement of TREK-1 from GM1 to PIP 2 clusters."
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"To test PIP 2 binding to TREK-1, we fused a nanoluciferase (Nluc) to the C terminus of the channel and identified a soluble fluorescent PIP 2 (FL-PIP 2 ) analog suitable for binding to TREK-1. xref shows a cartoon of the assay design."
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"Consistent with the ion flux data, ethanol had no effect on PIP 2 binding to TREK-1 or TRAAK (XREF_FIG) while norfluoxetine (NFX), a TREK-1 specific allosteric antagonist [XREF_BIBR], completely blocked PIP 2 binding (p < 0.0001) to TREK-1."
30529033
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"To eliminate the potential artifacts from the luciferase enzyme or the fluorophore attached to the probe, we confirmed PIP 2 binding to TREK-1 in a radioactive version of the lipid binding assay using a tritiated ( 3 H) PIP 2 and a scintillation proximity assay (SPA). xref shows binding of 3 H-PIP 2 to detergent-purified TREK-1 channel; FL-PIP 2 dose-dependently competed with 3 H-PIP 2 (K d , 0.80 μM; Hill slope, −0.85) (see also xref )."
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"We show that PIP 2 directly binds to TREK-1 and competes with lipid agonists PA and phosphatidylglycerol (PG) in purified liposomes."
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"The opposite effect of low and high levels of PIP 2 in the presence of PG ( xref and xref ) may suggest multiple sites for PIP 2 binding to TREK-1."
28793254
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"Consistent with the ion flux data, ethanol had no effect on PIP 2 binding to TREK-1 or TRAAK ( xref ) while norfluoxetine (NFX), a TREK-1 specific allosteric antagonist[ xref ], completely blocked PIP 2 binding (p<0.0001) to TREK-1."
30529033
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"Given that our soluble binding assay shows that PIP 2 binds the channel, we reasoned PIP 2 could bind and antagonize TREK-1."
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"However, the mechanisms by which regulatory lipids such as PIP 2 interact with TREK channels to influence these conformations remains unclear."
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"The direct binding of anionic lipids such as PA, phosphatidylglycerol (PG), and PIP to purified TREK-1 channels was demonstrated via a fluorescence binding assay (Cabanos et al., 2017) and to purified TRAAK channels by means of mass spectrometry (Schrecke et al., 2021)."
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"Collectively, these new data point out pCt as a major regulatory domain of these channels and suggest that the binding of PIP 2 to the pCt of TREK1 results in the stabilization of the conductive conformation in basal conditions."
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