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Astemizole inhibits KCNH1. 42 / 52
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"Small molecule EAG1 blockers such as astemizole have shown efficacy in reducing EAG1 expressing cancer cell growth in vitro and in vivo."
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"With the purpose of analyzing a possible synergistic effect upon proliferation by inhibiting Eag1 expression and channel activity, we incubated our cells in the presence of calcitriol and the Eag1 blo[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Treatment with astemizole was also shown to reduce the mRNA and protein expression levels of Eag1 in diethylnitrosamine-treated mice, resulting in both improved histological features and appearance of the liver (85)."
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"Unfortunately, all known hEag1 blockers (including imipramine and astemizole, [6–8] ) also inhibit HERG, which represents a serious difficulty for dissecting the functions of hEag1 and from a practica[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Astemizole permeates the cell membrane and inhibits Eag1 currents by selectively binding to open channels."
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"This cell line expresses Eag1, but not HERG (a relative of Eag1 that is very effectively blocked by astemizole and has also been implicated in tumor progression)."
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"Under these conditions, the double mutation increased the potency of hEag1 blockage by AST ( Table 2 and Fig. 2 B)."
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"In vivo, it was shown that the Kv10.1 blocker astemizole impaired MBCDF and T-47D cells xenografts growth."
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"HEag1 inhibition by the antihistamine astemizole, the tricyclic antidepressant imipramine or hEag1 specific monoclonal antibodies reduces tumor cell proliferation in vitro and in vivo [XREF_BIBR, XREF_BIBR, XREF_BIBR - XREF_BIBR]."
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"Astemizole inhibits Eag1 and Erg channel activity, and in cells expressing the Eag1 channel it decreases tumor cell proliferation in vitro and in vivo."
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"However, the fact that astemizole reduced Eag1 mRNA in this study might be secondary to H 1 receptor antagonism and subsequent inactivation of downstream signaling pathways associated with generation of second messengers and proliferation."
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"HEag1 inhibition by the antihistamine astemizole, the tricyclic antidepressant imipramine or hEag1 specific monoclonal antibodies reduces tumor cell proliferation in vitro and in vivo [ xref , xref , xref - xref ]."
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"Imipramine, a tryciclic antidepressant and the antihistamine astemizole inhibit eag1 [52,53] ; imipramine impairs cell proliferation in human melanoma cell lines expressing eag1 [52] ."
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"In striking contrast, although astemizole is a good inhibitor of hEAG1 (IC 50 196 nM), it is not a useful pharmacological tool for selectively probing hEAG1 function because it inhibits hERG with >200[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Since both astemizole and calcitriol inhibit EAG1 activity and expression, respectively, patients bearing EAG1 and VDR positive solid or metastatic tumors may benefit from this EAG1 double blocking strategy."
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"XREF_BIBR Thus, Eag1 channels are inhibited by astemizole and may be potential targets for cancer therapy."
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"Astemizole synergized calcitriol antiproliferative effects by downregulating CYP24A1, upregulating VDR and targeting Eag1."
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"Thus, the simultaneous inhibition of Kv10.1 and Kv11.1 by astemizole in AML cell types expressing both channels might be advantageous."
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"The small molecule EAG1 blocker astemizole reduced EAG1 expressing cancer cell growth in vitro and in vivo."
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"A possible role of hEag1 in leukemia cell proliferation could be shown by growth and migration inhibition of the hEag1 expressing cell lines PLB-985, K562, UT-7 and HEL and primary clinical samples by the potassium channel blockers astemizole, imipramine, the hEag1 specific monoclonal antibody mAb56 and siRNA knockdown [XREF_BIBR]."
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"Thus, we wondered whether two drugs that are widely used to inhibit Eag1, namely, astemizole and imipramine, might affect the cell proliferation of primary retinoblastoma cultures."
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"Inhibition of Eag1 by astemizole or by siRNA induced a decrease in cyclin D1 expression along with a strong decrease of pRb phosphorylation and an arrest of the cells in G1 phase of cell cycle."
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"Inhibition of Eag1 by astemizole or by siRNA induced a decrease in cyclin D1 expression along with a strong decrease of pRb phosphorylation and an arrest of the cells in G1 phase of cell cycle."
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"Interestingly, a nuclear localization sequence (NLS) has been found in Eag1 channels and currents resembling Eag1 channel activity blocked by astemizole have been recorded in the inner nuclear membrane [XREF_BIBR]."
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"EAG1 activity may be reduced by preventing its phosphorylation with epidermal growth factor receptor (EGFR) kinase inhibitors and by astemizole, which blocks the channel pore and downregulates its gene expression."
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"To demonstrate the inhibition of the hEag1 by astemizole we used a −60 mV holding potential where activation kinetics of the current is fast ( xref ) and consequently block equilibrium develops fast, reaching steady-state within 3000 ms at various concentrations of the drug ( xref B)."
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"Both outward and inward currents through channels that had constitutive activity could be blocked by the K V 10.1 blocker astemizole."
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"Astemizole can inhibit Eag1 and Erg channel activity and decrease tumor cell proliferation both in vitro and in vivo [XREF_BIBR]."
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"We interpret the increase in the Ca deposits as an indicator of an enhanced mineral matrix production of SaOS-2 cells when K channels are inhibited by 1 mM TEA.To analyze the contribution of hEag1 to the mineral matrix production of osteosarcoma cells, we used the hEag1 blocker astemizole."
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"Imipramine, a tryciclic antidepressant and the antihistamine astemizole inhibit eag1 [52,53] ; imipramine impairs cell proliferation in human melanoma cell lines expressing eag1 [52] ."
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"Open Channel Blockade of Eag1 Channels Reduces Tumor Progression in Vivo —Because inhibition of Eag1 by the open channel blockers astemizole and imipramine has been reported to inhibit proliferation of several cell types in vitro ( xref , xref ), we tested if similar effects could be observed in vivo ."
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"Suppression of Eag1 by astemizole or pKv10.1-3 sensitizes cells to TMZ."
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"At clinically achievable concentrations, astemizole synergized calcitriol antiproliferative effects by downregulating CYP24A1, upregulating VDR and targeting Eag1."
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"Astemizole, an anti-histamine, is able to inhibit both Kv10.1 and Kv11.1 channels, contributing to inhibition of cancer cell proliferation in vitro and in vivo [ xref , xref , xref ]."
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"The hEag1 blocker astemizole can increase the apoptotic response, inhibit cell migration in AML cells, and may serve as a potential target for treating AML (59)."
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"Considering previous research work from Camacho's group that Astemizole could inhibit tumor cell proliferation by targeting the EAG1 potassium channel [ 101 ], authors further investigated the linkage[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In combination with routinely used induction therapeutics, the hEag1 blockers astemizole and mAb56 were able to increase the apoptotic response in PLB-985 cells."
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"Dose dependent Inhibition of hEag1 Currents by Imipramine and Astemizole."
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"HEag1 channels recorded in these conditions were blocked by bath applications of imipramine (XREF_FIG A) and astemizole (XREF_FIG B)."
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"The steady-state current-voltage (I–V) relationship showed a strong outward rectification ( Fig. 2 C), and this current was inhibited by 200 nM astemizole (a specific inhibitor of Eag1 channel) ( Fig.[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Tumor growth induced by implantation of Eag1 expressing cells was clearly inhibited in the group treated with astemizole (XREF_FIG), similar to growth inhibition observed after treatment with the well established cytotoxic drug cyclophosphamide (CPM) (applied at the maximal tolerable dose of 5 mg/kg)."
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"This finding suggests either (a) that astemizole blocks hEag1 channels by binding in its uncharged form or (b) that the binding site lies out of the major drop of transmembrane potential."
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