IndraLab

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Phosphatidylinositol phosphate binds KCNK2. 8 / 8
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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."
28793254
sparser
"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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"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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"We show that PIP 2 directly binds to TREK-1 and competes with lipid agonists PA and phosphatidylglycerol (PG) in purified liposomes."
28793254
sparser
"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 )."
28793254
sparser
"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."
28793254
sparser
"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
sparser
"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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