IndraLab

Statements

Calcitriol inhibits KCNH1. 7 / 7
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"On the other hand, even if calcitriol consistently down-regulated Eag-1 in all cell lines tested, and the effect of both drugs combined upon inhibition of cell proliferation and Ki-67 expression was synergistic, the significant downregulation of Eag1 mRNA observed with the combination of astemizole plus calcitriol in IDC-1 was not detected in SUM-229PE cells."
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"In addition, calcitriol significantly inhibited tumoral EAG1 mRNA and protein expression, an effect that was further increased by the co-administration with astemizole, showing for the first time the in vivo inhibition of this oncogenic potassium channel by these drugs in breast tumors."
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"In these studies the calcitriol dependent downregulation of Eag1 was accompanied by inhibition of cell proliferation and reduction of tumor growth."
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"Calcitriol decreased EAG1 mRNA in all cell types, and EAG1 protein and proliferation in SiHa cells."
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"Therefore, the rationale of the combined therapy proposed herein is based on Eag1 gene expression inhibition by calcitriol, together with the functional blockade of K + currents through this particular channel by astemizole, in order to potentiate the antineoplastic effects of both compounds."
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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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"EAG1 mRNA was more potently inhibited by calcitriol in VDR transfected cells."
20682996