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PMID: 18523872
Muenster U, Grieshop B, Ickenroth K, Gnoth MJ
Characterization of substrates and inhibitors for the in vitro assessment of Bcrp mediated drug-drug interactions.
Pharm Res. 2008 Oct;25(10):2320-6. Epub 2008 Jun 4.,
[PubMed]
Sentences
No.
Mutations
Sentence
Comment
129
ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 18523872:129:89
status:
VERIFIED
view ABCG2 p.Arg482Gly details
Recently strong evidence for the existence of at least two separate binding sites in the
R482G
BCRP mutant has been presented (31).
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142
ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 18523872:142:113
status:
VERIFIED
view ABCG2 p.Arg482Thr details
Also Nakanishi et al. speculated a complex interaction of substrate with the BCRP transport protein (WT-BCRP and
R482T
variant), since in their substrate interaction studies using Rhodamin 123, topotecan, mitoxantrone, and flavopiridol, no two substrates reciprocally inhibited the efflux of the other (32).
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