ABCMdb

PMID: 18006847

Shi Z, Peng XX, Kim IW, Shukla S, Si QS, Robey RW, Bates SE, Shen T, Ashby CR Jr, Fu LW, Ambudkar SV, Chen ZS
Erlotinib (Tarceva, OSI-774) antagonizes ATP-binding cassette subfamily B member 1 and ATP-binding cassette subfamily G member 2-mediated drug resistance.
Cancer Res. 2007 Nov 15;67(22):11012-20., 2007-11-15 [PubMed]

Sentences

No. Mutations Sentence Comment

121 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly Recent studies have shown that mutations at amino acid 482 in ABCG2 affect the substrate and antagonist specificity of ABCG2 (23, 34); therefore, we investigated the reversal effect of erlotinib on both wild-type (R482) and mutated (R482G and R482T) ABCG2-mediated MDR. Login to comment 137 ABCG2 p.Arg482Gly These results suggest that erlotinib specifically potentiates the sensitivity of ABCB1 substrates in the ABCB1-overexpressing cells and also enhances the sensitivity of ABCG2 substrates in both wild-type and R482G/T mutant ABCG2-overexpressing cells we tested. Login to comment 211 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly In our results of transport by ABCG2 vesicles, E217hG and methotrexate are only transported by the wild-type ABCG2 and not by the two mutated R482G and R482T ABCG2. Login to comment 226 ABCG2 p.Gln141Lys ABCG2 p.Gln141Lys November 15, 2007 11018 www.aacrjournals.org American Association for Cancer ResearchCopyright (c) 2007 on May 3, Recently, Cusatis et al. (43) reported that one common functional single-nucleotide polymorphism in the ABCG2 gene, ABCG2 421C!A (Q141K), is associated with diarrhea, which is a gefitinib-induced adverse effect, and led to a high risk of diarrhea in patients treated with oral gefitinib. Login to comment