PMID: 15930306

Ahmed-Belkacem A, Pozza A, Munoz-Martinez F, Bates SE, Castanys S, Gamarro F, Di Pietro A, Perez-Victoria JM
Flavonoid structure-activity studies identify 6-prenylchrysin and tectochrysin as potent and specific inhibitors of breast cancer resistance protein ABCG2.
Cancer Res. 2005 Jun 1;65(11):4852-60., 2005-06-01 [PubMed]
Sentences
No. Mutations Sentence Comment
10 ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 15930306:10:4
status: VERIFIED
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 The R482T mutation limited the effect of prenylation on ABCG2 inhibition. Login to comment 24 ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 15930306:24:204
status: VERIFIED
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ABCG2 p.Arg482Gly
X
ABCG2 p.Arg482Gly 15930306:24:213
status: VERIFIED
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 The precise substrate profile depends on a hotspot mutation at position 482 such that methotrexate is only transported by wild-type ABCG2 (R482) and anthracyclines and rhodamine 123 only by mutant ABCG2 (R482T or R482G), whereas Hoechst33342 and mitoxantrone are transported by all variants (9). Login to comment 40 ABCG2 p.Arg482Thr
X
ABCG2 p.Arg482Thr 15930306:40:19
status: VERIFIED
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 Interestingly, the R482T mutation limited this prenylation-dependent effect, whereas the inhibitory potency of tectochrysin was even increased, especially towards rhodamine transport. Login to comment