IndraLab

Statements

Astemizole inhibits KCNH1. 38 / 41
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"Astemizole synergized calcitriol antiproliferative effects by downregulating CYP24A1, upregulating VDR and targeting Eag1."
22984610
sparser
"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."
23970866
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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)."
15365094
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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]."
20105281
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"XREF_BIBR Thus, Eag1 channels are inhibited by astemizole and may be potential targets for cancer therapy."
27703327
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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."
25049269
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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."
28360219
dgi
No evidence text available
ctd
No evidence text available
14985237
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"Suppression of Eag1 by astemizole or pKv10.1-3 sensitizes cells to TMZ."
27698831
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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]."
20105281
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"Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide."
16949586
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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."
31973216
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"The small molecule EAG1 blocker astemizole reduced EAG1 expressing cancer cell growth in vitro and in vivo."
25852478
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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]."
22778627
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"Astemizole permeates the cell membrane and inhibits Eag1 currents by selectively binding to open channels."
22984610
ctd
No evidence text available
16816845
ctd
No evidence text available
20050851
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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)."
18927085
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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."
15365094
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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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"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]"
19932096
ctd
No evidence text available
18497958
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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)."
18927085
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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."
23970866
sparser
"Thus, the simultaneous inhibition of Kv10.1 and Kv11.1 by astemizole in AML cell types expressing both channels might be advantageous."
35207698
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"Here, the authors showed that inhibition of KV10.1 by astemizole in T-84 cells inhibits pHi regeneration after an NH4+ prepulse, which points to an inhibition of the H+ extrusion pathways upon K+ channel inhibition."
32887220
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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."
20105281
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"Dose dependent Inhibition of hEag1 Currents by Imipramine and Astemizole."
15365094
sparser
"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 ]."
20105281
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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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"In vivo, it was shown that the Kv10.1 blocker astemizole impaired MBCDF and T-47D cells xenografts growth."
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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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"At clinically achievable concentrations, astemizole synergized calcitriol antiproliferative effects by downregulating CYP24A1, upregulating VDR and targeting Eag1."
22984610
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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 ]."
26010603
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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]."
26830359
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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."
21443504
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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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