IndraLab

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Probucol activates KCNH2. 8 / 8
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"While progesterone induces ER stress leading to blockade of K v 11.1 maturation ( Wu et al., 2011 ), probucol increases endocytotic uptake and subsequent degradation of K v 11.1 protein by increasing [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Its inhibitory effect is reversed in the presence of pharmacological chaperones, astemizole and dofetilide, suggesting that pentamidine and pharmacological chaperones compete for the same binding site[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"This seems to be a result of enhanced degradation of plasma membrane hERG protein induced by probucol treatment."
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"Likewise, CCh (25 and 50 muM) reversed the downregulation of I hERG induced by 100 muM probucol (XREF_FIG)."
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"Therefore, these results demonstrate that matrine and oxymatrine could rescue probucol induced hERG deficiency, which may lead to potentially effective clinical therapeutic drugs for treating cardiotoxicity in the future."
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"We also demonstrated that matrine and oxymatrine were able to upregulate Sp1 expression which may be one of the possible mechanisms that by which matrine and oxymatrine rescued probucol induced hERG channel deficiency."
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"To identify the damage of hERG current induced by probucol depended on the decrease of protein level but not channel functions, patch-clamp recordings were used to detect the long-term effect of probucol on hERG-channel kinetics."
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"On the contrary, carbachol could enhance the phosphorylation level of Nedd4-2 as an alternative to SGK1, and thus rescue the ubiquitin mediated degradation of hERG channels caused by probucol."
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