ABCMdb

PMID: 19148526

Shi Z, Parmar S, Peng XX, Shen T, Robey RW, Bates SE, Fu LW, Shao Y, Chen YM, Zang F, Chen ZS
The epidermal growth factor tyrosine kinase inhibitor AG1478 and erlotinib reverse ABCG2-mediated drug resistance.
Oncol Rep. 2009 Feb;21(2):483-9., [PubMed]

Sentences

No. Mutations Sentence Comment

67 ABCG2 p.Arg482Thr ABCG2 p.Arg482Gly Since mutations at amino acid 482 of ABCG2 could alter the substrate and antagonist specificity of ABCG2 (26,27), we examined the potential impact of mutation at this site on the effects of AG1478 and erlotinib by performing studies on cells overexpressing wild-type (R482) ABCG2-overexpressing MCF-7/FLV1000, mutant ABCG2-overexpressing MCF-7/AdVp3000 (R482T) and S1-M1-80 (R482G). Login to comment 149 ABCG2 p.Gln141Lys One common single-nucleotide polymorphism of ABCG2 that has been shown to affect the function of ABCG2, Q141K (421Cėd;A), was reported to be associated with gefitinib-induced diarrhea, resulting in a high risk of diarrhea in patients treated with oral gefitinib (36), and was also found to be associated with greater accumulation at steady-state and toxicity of gefitinib (37). Login to comment