bcrp - publications

Predict more bcrp - ligand interactions now!


1. Mol Med Report. 2012 Mar;5(3):603-9. doi: 10.3892/mmr.2011.734. Epub 2011 Dec 22.

Differential effects of calcium antagonists on ABCG2/BCRP-mediated drug
resistance and transport in SN-38-resistant HeLa cells.

Takara K, Matsubara M, Yamamoto K, Minegaki T, Takegami S, Takahashi M, Yokoyama
T, Okumura K.

Department of Clinical Pharmaceutics, Faculty of Pharmaceutical Sciences, Himeji
Dokkyo University, Himeji 670-8524, Japan. takara@gm.himeji-du.ac.jp

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.

PMID: 22200670 [PubMed - in process]