IndraLab

Statements

PD-118057 activates KCNH2. 6 / 6
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"We conclude that direct interaction of PD-118057 with the pore helix attenuates fast P-type inactivation and increases open probability of hERG1 channels."
19892732
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"It had been previously established by experiment that PD-118057 and ICA-105574, drugs that inhibits inactivation and thus increase hERG current, bind near F619 and L622 XREF_BIBR, XREF_BIBR."
22848423
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"Although recent studies can not rule out the possibility that PD-118057 acts through indirect mechanisms to increase hERG currents, our results showing the failure of PD-118057 to significantly affect the gating and kinetic properties of the hERG channel cause us to speculate that PD-118057 increases current amplitude by binding to the channel directly and increasing its open probability and activation potential."
23840331
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"PD-118057 enhances hERG1 current by increasing channel open probability and causing a positive shift in the voltage dependence of inactivation 80."
27261821
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"PD-118057 increases the channel-open probability of Kv11.1 and shifts its voltage dependence of inactivation to more positive potentials [ 74 ], while RPR-260243 slows the rate of Kv11.1 channel deact[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
33858691
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"In contrast, PD-307243, a structure analog of PD-118057, increased hERG current with the rates of both inactivation and deactivation being slowed markedly [16] ."
19426677