https://scholars.lib.ntu.edu.tw/handle/123456789/191077
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor | 臺大醫院-內科部;臺大醫學院;臺大醫學院-毒理學研究所; | - |
dc.contributor.author | Wada, Koji | en_US |
dc.contributor.author | Lee, Jen-Yi | en_US |
dc.contributor.author | Hung, Hsin-Yi | en_US |
dc.contributor.author | Shi, Qian | en_US |
dc.contributor.author | Lin, Li | en_US |
dc.contributor.author | Zhao, Yu | en_US |
dc.contributor.author | Goto, Masuo | en_US |
dc.contributor.author | PAN-CHYR YANG | en_US |
dc.contributor.author | Kuo, Sheng-Chu | en_US |
dc.contributor.author | HUEI-WEN CHEN | en_US |
dc.contributor.author | Lee, Kuo-Hsiung | en_US |
dc.creator | Wada, Koji;Lee, Jen-Yi;Hung, Hsin-Yi;Shi, Qian;Lin, Li;Zhao, Yu;Goto, Masuo;Yang, Pan-Chyr;Kuo, Sheng-Chu;Chen, Hui-Wen;Lee, Kuo-Hsiung | en |
dc.creator | 楊泮池;陳惠文 | zh-tw |
dc.date | 2015 | - |
dc.date.accessioned | 2017-05-26T04:11:19Z | - |
dc.date.accessioned | 2018-07-11T07:12:03Z | - |
dc.date.available | 2017-05-26T04:11:19Z | - |
dc.date.available | 2018-07-11T07:12:03Z | - |
dc.date.issued | 2015 | - |
dc.identifier.uri | http://ntur.lib.ntu.edu.tw//handle/246246/279062 | - |
dc.description.abstract | Curcumin (1) down-regulates the expression as well as phosphorylation of epidermal growth factor receptor (EGFR) in lung adenocarcinoma cells expressing gefitinib-resistant EGFR. Thirty-seven newly synthesized curcumin analogues including dimethoxycurcumin (2, DMC) were evaluated for their effects on EGFR expression as well as phosphorylation in two gefitinib-resistant lung adenocarcinoma cell lines, CL1-5 (EGFR(wt)) and H1975 (EGFR(L858R+T790M)). Based on the identified structure-activity relationships, methoxy substitution at C-3', C-4', or both positions favored inhibitory activity (compounds 1, 2, 5, 815, 17, 36), while compounds with more polar substituents were generally less active in both cell lines. Compound 36 with a fluorine substituent at C-6' and its protonated counterpart 2 did not lose activity, suggesting halogen tolerance. In addition, a conjugated linker was essential for activity. Among all evaluated curcumin derivatives, compound 2 showed the best inhibitory effects on both wild-type and mutant EGFR by efficiently inducing gefitinib-insensitive EGFR degradation. Compound 23 also reduced gefitinib-induced gastrointestinal damage in the non-transformed intestinal epithelial cell line IEC-18. (C) 2015 Elsevier Ltd. All rights reserved. | en_US |
dc.language | en-us | - |
dc.relation | Bioorg. Med. Chem., 23(7), 1507-1514 | en_US |
dc.relation.ispartof | Bioorg. Med. Chem. | en_US |
dc.subject | Curcumin | en_US |
dc.subject | EGFR | en_US |
dc.subject | Gastrointestinal tract | en_US |
dc.subject | Lung adenocarcinoma | en_US |
dc.subject | Tyrosine kinase inhibitor | en_US |
dc.subject.classification | [SDGs]SDG3 | - |
dc.subject.other | curcumin; curcumin derivative; dimethoxycurcumin; epidermal growth factor receptor; gefitinib; unclassified drug; curcumin; EGFR protein, human; epidermal growth factor receptor; protein kinase inhibitor; Article; cancer cell line; cell proliferation; controlled study; digestive system injury; down regulation; drug determination; drug synthesis; human; human cell; lung adenocarcinoma; physical parameters; protein degradation; protein expression; protein phosphorylation; structure activity relation; adenocarcinoma; analogs and derivatives; antagonists and inhibitors; chemically induced; chemistry; drug effects; drug resistance; drug screening; gastrointestinal disease; immunology; Lung Neoplasms; metabolism; procedures; tumor cell line; Adenocarcinoma; Cell Line, Tumor; Curcumin; Drug Resistance, Neoplasm; Gastrointestinal Diseases; Humans; Lung Neoplasms; Protein Kinase Inhibitors; Receptor, Epidermal Growth Factor; Xenograft Model Antitumor Assays | - |
dc.title | Novel curcumin analogs to overcome EGFR-TKI lung adenocarcinoma drug resistance and reduce EGFR-TKI-induced GI adverse effects | en_US |
dc.identifier.doi | 10.1016/j.bmc.2015.02.003 | - |
dc.relation.pages | 1507-1514 | en_US |
dc.relation.journalvolume | 23 | en_US |
dc.relation.journalissue | 7 | en_US |
item.fulltext | no fulltext | - |
item.grantfulltext | none | - |
crisitem.author.dept | Internal Medicine | - |
crisitem.author.dept | Clinical Medicine | - |
crisitem.author.dept | Clinical Pharmacy | - |
crisitem.author.dept | Oncology | - |
crisitem.author.dept | Biomedical Electronics and Bioinformatics | - |
crisitem.author.dept | Internal Medicine-NTUH | - |
crisitem.author.dept | Toxicology | - |
crisitem.author.dept | Genome and Systems Biology Degree Program | - |
crisitem.author.orcid | 0000-0001-6330-6048 | - |
crisitem.author.orcid | 0000-0001-5051-9896 | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Electrical Engineering and Computer Science | - |
crisitem.author.parentorg | National Taiwan University Hospital | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Life Science | - |
顯示於: | 醫學系 |
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