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BBR inhibits KCNH2. 16 / 16
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"In this report, we tested three drugs for their ability to rescue BBR-induced hERG inhibition."
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"In summary, we clarified that disruption of cav-1 and binding to the residues, Tyr652 and Phe656, are responsible for BBR induced hERG reduction on the membrane, which contribute to better understanding of the mechanisms underlying drug induced LQTS."
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"Previous report illustrated that BBR acutely block hERG channel by interacting with specific residues (Tyr652 and Phe656)."
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"XREF_BIBR However, there was no report to elucidate that the binding sites mediate hERG reduction triggered by BBR incubation."
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"BBR decreased the expression of cav-1 (XREF_FIG) and knocking down the basal expression of cav-1 alleviated BBR induced hERG decrease on plasma membrane (XREF_FIG)."
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"At concentrations similar to the IC 50 of = ~ 3 microM for CGN viability, BBR inhibits delayed rectifier currents and HERG channels XREF_BIBR, XREF_BIBR, XREF_BIBR."
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"XREF_BIBR Hence, we conclude that BBR reduces surface hERG protein through promoting hERG internalization due to its co-localization with cav-1 on the membrane."
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"As shown in xref , the fully glycosylated 155 kDa hERG protein inhibited by 10 μM BBR was successfully restored by all these drugs and there was no distinct difference among their ability to rescue hERG trafficking."
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"Considering both our previous and present work, we propose that BBR reduces hERG membrane stability with multiple mechanisms."
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"Previous researches showed that BBR acutely blocks hERG channel in Xenopus oocytes by interacting with the two aromatic amino acid residues (tyrosine [Tyr652] and phenylalanine [Phe656], which are thought as the universal binding sites for various hERG channel blockers) located in S6 transmembrane helix."
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"Previous studies have demonstrated that BBR blocks hERG channels and prolongs action potential duration (APD)."
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"BBR inhibited hERG channel on membrane via cav-1 interference."
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"It has been confirmed that BBR could block the hERG channel and prolong action potential duration (APD) [XREF_BIBR, XREF_BIBR]."
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"Knocking down the basal expression of caveolin-1 alleviates BBR induced hERG reduction."
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"BBR has been reported previously to block hERG currents expressed in HEK-293 cells and Xenopus oocytes after acute application."
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"XREF_BIBR Recently, we found that long-term application of BBR induced hERG channel reduction by disrupting channel trafficking."
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