PMID: 24726739

Zhang H, Kathawala RJ, Wang YJ, Zhang YK, Patel A, Shukla S, Robey RW, Talele TT, Ashby CR Jr, Ambudkar SV, Bates SE, Fu LW, Chen ZS
Linsitinib (OSI-906) antagonizes ATP-binding cassette subfamily G member 2 and subfamily C member 10-mediated drug resistance.
Int J Biochem Cell Biol. 2014 Jun;51:111-9. doi: 10.1016/j.biocel.2014.03.026. Epub 2014 Apr 12., [PubMed]
Sentences
No. Mutations Sentence Comment
134 ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 24726739:134:252
status: NEW
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ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 24726739:134:216
status: NEW
view ABCG2 p.Arg482Gly details
 Thus, in order to determine whether linsitinib increases the drug sensitivity in both wild-type and mutant ABCG2-overexpressing cells, we used HEK293 transfected wild-type ABCG2-482-R2 (Arg482), mutant ABCG2-482-G2 (Arg482Gly) and mutant ABCG2-482-T7 (Arg482Thr) cell lines. Login to comment 144 ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 24726739:144:91
status: NEW
view ABCG2 p.Arg482Gly details
 These results indicated that linsitinib inhibits the activity of both wild-type and mutant Arg482Gly/Thr ABCG2. Login to comment