Document Detail


Sensitivity and kinase activity of epidermal growth factor receptor (EGFR) exon 19 and others to EGFR-tyrosine kinase inhibitors.
MedLine Citation:
PMID:  23387505     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
The presence of epidermal growth factor receptor (EGFR) somatic mutations in non-small cell lung cancer patients is associated with response to treatment with EGFR-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib and erlotinib. More than one hundred mutations in the kinase domain of EGFR have been identified. In particular there are many variations of deletion mutations in exon 19. In this study, we examined the differences in sensitivity to gefitinib, erlotinib and afatinib of several exon 19 mutants and other common EGFR mutations, using YFP-tagged fragments of the EGFR intracellular domain. We also used serum of patients undergoing treatment with EGFR-TKIs in this system. In addition, we examined the relative kinase activity of these mutants by measurement of the relative fluorescent intensity after immunofluorescence staining. We found that both sensitivity to EGFR-TKIs and relative kinase activity differed among several EGFR mutations found in the same region of the kinase domain. This study underscores the importance of reporting the clinical outcome of treatment in relation to different EGFR mutations.
Authors:
Kazuto Furuyama; Taishi Harada; Eiji Iwama; Yoshimasa Shiraishi; Kyoko Okamura; Kayo Ijichi; Akiko Fuj; Keiichi Ota; Shuo Wang; Heyan Li; Koichi Takayama; Giuseppe Giaccone; Yoichi Nakanishi
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-2-7
Journal Detail:
Title:  Cancer science     Volume:  -     ISSN:  1349-7006     ISO Abbreviation:  Cancer Sci.     Publication Date:  2013 Feb 
Date Detail:
Created Date:  2013-2-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101168776     Medline TA:  Cancer Sci     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
© 2013 Japanese Cancer Association.
Affiliation:
Research Institute for Diseases of the Chest, Graduate School of Medical Sciences, Kyushu University, Fukuoka, Japan.
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