Title : Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan.

Pub. Date : 2006 Sep

PMID : 16404634






6 Functional Relationships(s)
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1 Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Sirolimus ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
2 Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Sirolimus ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
3 Therefore, the aim of this study was to determine whether the immunosuppressants cyclosporin A, tacrolimus and sirolimus are inhibitors and/or substrates of BCRP. Sirolimus ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
4 RESULTS: Cyclosporin A, tacrolimus and sirolimus significantly inhibited BCRP-mediated efflux of pheophorbide A, mitoxantrone and BODIPY-prazosin. Sirolimus ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
5 The EC(50) values of cyclosporin A, tacrolimus and sirolimus for inhibition of BCRP-mediated pheophorbide A efflux were 4.3 +/- 1.9 microM, 3.6 +/- 1.8 microM and 1.9 +/- 0.4 microM, respectively. Sirolimus ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
6 Cyclosporin A, tacrolimus and sirolimus also effectively reversed resistance of HEK cells to topotecan and mitoxantrone conferred by BCRP. Sirolimus ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens