Abstract:
: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.
journal_name
Mol Med Repjournal_title
Molecular medicine reportsauthors
Takara K,Matsubara M,Yamamoto K,Minegaki T,Takegami S,Takahashi M,Yokoyama T,Okumura Kdoi
10.3892/mmr.2011.734subject
Has Abstractpub_date
2012-03-01 00:00:00pages
603-9issue
3eissn
1791-2997issn
1791-3004journal_volume
5pub_type
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