PMID: 24747122

Zhang H, Wang YJ, Zhang YK, Wang DS, Kathawala RJ, Patel A, Talele TT, Chen ZS, Fu LW
AST1306, a potent EGFR inhibitor, antagonizes ATP-binding cassette subfamily G member 2-mediated multidrug resistance.
Cancer Lett. 2014 Aug 1;350(1-2):61-8. doi: 10.1016/j.canlet.2014.04.008. Epub 2014 Apr 18., [PubMed]
Sentences
No. Mutations Sentence Comment
86 ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 24747122:86:182
status: NEW
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ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 24747122:86:168
status: NEW
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 Therefore, we investigated whether AST1306 could reverse ABCG2-mediated resistance to its substrates in cells transfected with either the wild-type (Arg482) or mutant (Arg482Gly and Arg482Thr) forms of ABCG2. Login to comment 87 ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 24747122:87:331
status: NEW
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 As shown in Table 2, AST1306 could significantly increase sensitivity to MX and SN-38 in ABCG2-482-R2, ABCG2-482-G2 and ABCG2-482-T7 cells, respectively, and this effect was similar to that obtained with 1 lM FTC. These results indicated that AST1306 can reverse ABCG2-mediated MDR in cells expressing either wild-type or mutant Arg482Gly/Thr ABCG2 (Table 2). Login to comment