ABCMdb

PMID: 22778153

Sen R, Natarajan K, Bhullar J, Shukla S, Fang HB, Cai L, Chen ZS, Ambudkar SV, Baer MR
The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the MDR-associated ATP-binding cassette transporter ABCG2.
Mol Cancer Ther. 2012 Sep;11(9):2033-44. doi: 10.1158/1535-7163.MCT-12-0302. Epub 2012 Jul 9., [PubMed]

Sentences

No. Mutations Sentence Comment

25 ABCG2 p.Arg482Thr Doxorubicin- and verapamil-selected MCF7/AdrVp breast carcinoma cells, overexpressing ABCG2 with the R482T mutation (25), were obtained from Dr. Douglas Ross, University of Maryland Greenebaum Cancer Center, Baltimore, MD, and flavopiridol-selected MCF-7/Flv1000 cells (26), overexpressing wild-type ABCG2, from Dr. Susan Bates, National Cancer Institute. Login to comment 27 ABCG2 p.Arg482Thr Doxorubicin- and verapamil-selected MCF7/AdrVp breast carcinoma cells, overexpressing ABCG2 with the R482T mutation (25), were obtained from Dr. Douglas Ross, University of Maryland Greenebaum Cancer Center, Baltimore, MD, and flavopiridol-selected MCF-7/Flv1000 cells (26), overexpressing wild-type ABCG2, from Dr. Susan Bates, National Cancer Institute. Login to comment 67 ABCG2 p.Arg482Thr The effect in MCF7/AdrVp was less than in 8226/MR20 and K562/ABCG2, likely because of a greater degree of resistance in the solid tumor in relation to hematopoietic cell lines, rather than to the presence of the R482T mutation in MCF7/AdrVp, though the latter is also possible. Login to comment 68 ABCG2 p.Arg482Thr Because the R482T ABCG2 mutation is not clinically relevant, we did not pursue this distinction. Login to comment 69 ABCG2 p.Arg482Thr The effect in MCF7/AdrVp was less than in 8226/MR20 and K562/ABCG2, likely because of a greater degree of resistance in the solid tumor in relation to hematopoietic cell lines, rather than to the presence of the R482T mutation in MCF7/AdrVp, though the latter is also possible. Login to comment 70 ABCG2 p.Arg482Thr Because the R482T ABCG2 mutation is not clinically relevant, we did not pursue this distinction. Login to comment