ABCMdb

PMID: 18271955

Tang R, Faussat AM, Perrot JY, Marjanovic Z, Cohen S, Storme T, Morjani H, Legrand O, Marie JP
Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML).
BMC Cancer. 2008 Feb 13;8:51., [PubMed]

Sentences

No. Mutations Sentence Comment

21 ABCG2 p.Arg482Thr In contrast, zosuquidar, a highly specific P-gp inhibitor, which does not interact with other transporters including MRP1, MRP2 and mutant BCRP (R482T) [12], has been developed in an attempt to avoid significant pharmacokinetic interactions and therefore allow co-administration of standard dosing of cytotoxic chemotherapy. Login to comment 88 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly Lack of effect of zosuquidar on wild type BCRP-expressing cells Daunorubicin and idarubicin are transported by mutant BCRP (R482T or R482G) and not by wild type BCRP (R482), while mitoxantrone is transported by all BCRP variants [20]. Login to comment 89 ABCG2 p.Arg482Thr It has been shown that zosuquidar did not affect on the mutant BCRP (R482T) mediated drug transport [21]. Login to comment 120 ABCG2 p.Arg482Thr It has been shown that zosuquidar did not affect on the mutant BCRP (R482T) mediated drug transport [21]. Login to comment