IndraLab

Statements


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"Anson et al. [XREF_BIBR] demonstrated that RTV, LPV, NFV, and saquinavir substantially suppress HERG currents expressed in HEK293 cells and the corresponding endogenous current, I Kr, in mouse neonatal myocytes."

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"In silico test to measure whether Saquinavir and its analogs may (not) block the HERG K + ion channels of the heart suggest S2 to be a better molecule with minimum HERG inhibition value of 0.12 followed by S1 (0.13) and Saquinavir drug (0.14)."

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"In vitro, lopinavir, nelfinavir, ritonavir, and saquinavir caused dose dependent hERG channel blockade."

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"Thus, a potentially complex contribution and interplay between direct hERG blocking and hERG trafficking by saquinavir may potentially contribute to the day-to-day variability seen in mean maximum incrementQTcF dense."

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"Drug induced QT prolongation is usually caused by block of human ether-a-go-go-related gene (HERG) potassium channels, and we showed that lopinavir, nelfinavir, ritonavir, and saquinavir caused dose dependent block of HERG channels heterologously expressed in HEK293 cells in vitro."