PMID: 14500392

Volk EL, Schneider E
Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter.
Cancer Res. 2003 Sep 1;63(17):5538-43., 2003-09-01 [PubMed]
Sentences
No. Mutations Sentence Comment
29 ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 14500392:29:254
status: VERIFIED
view ABCG2 p.Arg482Thr details
ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 14500392:29:264
status: VERIFIED
view ABCG2 p.Arg482Gly details
 Together, these data suggested that BCRP can function as a MTX transporter. However, resistance to MTX occurred only in the presence of the wild-type transporter, which contains an arginine at position 482, whereas cells that overexpress a mutated BCRP (R482T and R482G) remained sensitive to MTX. Login to comment 171 ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 14500392:171:81
status: VERIFIED
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 In contrast, no uptake of MTX was observed into vesicles containing BCRP with an R482G mutation. Login to comment 174 ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 14500392:174:26
status: VERIFIED
view ABCG2 p.Arg482Gly details
 Thus, it appears that the R482G mutation resulted in a dramatic change in substrate specificity for BCRP. Login to comment