TY - JOUR AB - The effects of 9 calcium antagonists on ABCG2/BCRP-mediated resistance and transport were examined in HeLa and SN-38-resistant HeLa (HeLa/SN100) cells, overexpressing ABCG2/BCRP. Sensitivity to mitoxantrone, an ABCG2/BCRP substrate, in HeLa/SN100 cells was significantly reversed by the coexistence of the calcium antagonists, except for diltiazem and verapamil. The accelerated transport activity of Hoechst33342, an ABCG2/BCRP substrate, in HeLa/SN100 cells was significantly decreased by the presence of the calcium antagonists, except for diltiazem, nifedipine or verapamil, returning to the level of HeLa cells. The present study classifies the calcium antagonists into 3 categories: strong (benidipine, felodipine, nicardipine, nisoldipine and nitrendipine), moderate (amlodipine and nifedipine) and weak (diltiazem and verapamil) inhibitors of ABCG2/BCRP. AD - Department of Clinical Pharmaceutics, Faculty of Pharmaceutical Sciences, Himeji Dokkyo University, Himeji 670-8524, Japan Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8414, Japan Department of Analytical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8414, Japan AU - Takara,Kohji AU - Matsubara,Mika AU - Yamamoto,Kazuhiro AU - Minegaki,Tetsuya AU - Takegami,Shigehiko AU - Takahashi,Minoru AU - Yokoyama,Teruyoshi AU - Okumura,Katsuhiko DA - 2012/03/01 DO - 10.3892/mmr.2011.734 EP - 609 IS - 3 JO - Mol Med Rep KW - calcium antagonist ABCG2/BCRP drug resistance transport HeLa PY - 2012 SN - 1791-2997 1791-3004 SP - 603 ST - Differential effects of calcium antagonists on ABCG2/BCRP-mediated drug resistance and transport in SN-38-resistant HeLa cells T2 - Molecular Medicine Reports TI - Differential effects of calcium antagonists on ABCG2/BCRP-mediated drug resistance and transport in SN-38-resistant HeLa cells UR - https://doi.org/10.3892/mmr.2011.734 VL - 5 ER -