PMID: 23153455

Wu CP, Sim HM, Huang YH, Liu YC, Hsiao SH, Cheng HW, Li YQ, Ambudkar SV, Hsu SC
Overexpression of ATP-binding cassette transporter ABCG2 as a potential mechanism of acquired resistance to vemurafenib in BRAF(V600E) mutant cancer cells.
Biochem Pharmacol. 2013 Feb 1;85(3):325-34. doi: 10.1016/j.bcp.2012.11.003. Epub 2012 Nov 12., [PubMed]
Sentences
No. Mutations Sentence Comment
78 ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 23153455:78:230
status: NEW
view ABCG2 p.Arg482Gly details
ABCG2-mediated efflux of PhA was inhibited significantly by vemurafenib (2 mM) in ABCG2-overexpressing HEK293 (Fig. 1A), MCF7-FLV1000 (wild type R482) (Fig. 1B, middle panel),MCF7-AdVp3000(R482 T)(Fig1B, rightpanel) and S1-M1-80 (R482G) (Fig. 1 C) MDR cancer cell lines. Login to comment
98 ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 23153455:98:128
status: NEW
view ABCG2 p.Arg482Thr details
ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 23153455:98:150
status: NEW
view ABCG2 p.Arg482Gly details
The levels of accumulated fluorescent PhA in ABCG2-overexpressing (A) R482-HEK293, (B) MCF7-FLV1000 (wild-type), MCF7-AdVp3000 (R482T), (C) S1-M1-80 (R482G) cells and drug-sensitive parental cells or (D) concentration-dependent inhibition of ABCG2-mediated efflux of mitoxantrone by increasing concentrations of vemurafenib in MCF7-FLV1000 (*), MCF7-AdVp3000 (*) and S1-M1-80 (&) cells. Login to comment