ABCMdb

PMID: 18829547

Dai CL, Tiwari AK, Wu CP, Su XD, Wang SR, Liu DG, Ashby CR Jr, Huang Y, Robey RW, Liang YJ, Chen LM, Shi CJ, Ambudkar SV, Chen ZS, Fu LW
Lapatinib (Tykerb, GW572016) reverses multidrug resistance in cancer cells by inhibiting the activity of ATP-binding cassette subfamily B member 1 and G member 2.
Cancer Res. 2008 Oct 1;68(19):7905-14., 2008-10-01 [PubMed]

Sentences

No. Mutations Sentence Comment

175 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly Therefore, we investigated whether lapatinib would reverse ABCG2-mediated resistance to mitoxantrone in cells transfected with either the wild-type (R482) or mutant (R482G and R482T) forms of ABCG2. Login to comment 181 ABCG2 p.Arg482Gly These results suggest that lapatinib specifically enhances the sensitivity of ABCG2 substrates in cells expressing either wild-type or mutant R482G/T ABCG2. Login to comment 307 ABCG2 p.Gln141Lys Recently, Cusatis and colleagues (45) reported that one common functional single-nucleotide polymorphism in the ABCG2 gene, ABCG2 421C!A (Q141K), is associated with diarrhea, a gefitinib-induced adverse effect, and led to a high risk of diarrhea in patients treated with oral gefitinib. Login to comment 314 ABCG2 p.Arg482Gly Our results showed that lapatinib significantly enhances the sensitivity of ABCG2 substrates not only in cells overexpressing wild-type but also in the R482G/T variants of ABCG2. Login to comment