IndraLab

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"Finally, antagonism of doxazosin induced hERG protein suppression and glioblastoma cell death by co-treatment of terazosin and doxazosin indicates the functional relevance of hERG protein in GB cell apoptosis."

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"Doxazosin can directly block the activity of hERG, and this effect is related to KCNH2 polymorphisms."

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"In conclusion, this study demonstrates that HERG potassium channels are blocked by prazosin, doxazosin, and terazosin."

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"XREF_BIBR reported that doxazosin can directly block KCNH2, and the sensitivity is influenced by the mutation of KCNH2 (1956, C> T), while other research found that celiprolol involved in modulating the function of endothelial cells and had certain antioxidant stress effects XREF_BIBR, XREF_BIBR."

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"The antihypertensive agent, doxazosin pharmacologically blocks the hERG channel [XREF_BIBR]."

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"Previous studies have reported that the expression of hERG channels in a variety of tumor cells could facilitate cell proliferation [47,48,85], and doxazosin inhibits hERG currents to reduce the proliferation of tumor cells [86,87]."

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"An unexpected finding was revealed : simultaneous application of 100 microM terazosin attenuated doxazosin induced hERG suppression to 24.5 +/-11.4% (n = 3; p = 0.07; XREF_FIG)."

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"29 In addition, hERG blockers doxazosin and terazosin did not cause cell cycle arrest despite hERG expression in distinct cell lines, for example, LNCaP prostate carcinoma cells."

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"Given that GB cells express hERG channels and that hERG suppression by doxazosin induces apoptosis, we hypothesized that pharmacological targeting of hERG channels would induce apoptosis of GB cells."

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"Furthermore, additional reduction of hERG viability in the presence of anti-HERG siRNA may be caused by doxazosin induced suppression of residual hERG protein (~ 42%)."

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"The hERG blocker doxazosin has been proven as a proapoptotic agent in a wide range of in vitro and in vivo studies."

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"Inhibition of hERG by doxazosin, an antihypertensive drug, has been shown to promote apoptosis by a not fully clarified mechanism [49] ."