Astemizole Synergizes Calcitriol Antiproliferative Activity by Inhibiting CYP24A1 and Upregulating VDR: A Novel Approach for Breast Cancer Therapy

作者: Janice García-Quiroz , Rocío García-Becerra , David Barrera , Nancy Santos , Euclides Avila

DOI: 10.1371/JOURNAL.PONE.0045063

关键词: Cell growthBreast cancerCYP24A1Calcitriol receptorAstemizoleDownregulation and upregulationCalcitriolPharmacologyChemistryCarcinogenesisGeneral Biochemistry, Genetics and Molecular BiologyGeneral Agricultural and Biological SciencesGeneral Medicine

摘要: Background Calcitriol antiproliferative effects include inhibition of the oncogenic ether-a-go-go-1 potassium channel (Eag1) expression, which is necessary for cell cycle progression and tumorigenesis. Astemizole, a new promising antineoplastic drug, targets Eag1 by blocking ion currents. Herein, we characterized interaction between calcitriol astemizole as well their conjoint action in SUM-229PE, T-47D primary tumor-derived breast cancer cells.

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