https://scholars.lib.ntu.edu.tw/handle/123456789/626950
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor.author | Lin, Ming-Shiu | en_US |
dc.contributor.author | Hong, Tse-Ming | en_US |
dc.contributor.author | Chou, Ting-Hung | en_US |
dc.contributor.author | Yang, Shuenn-Chen | en_US |
dc.contributor.author | Chung, Wei-Chia | en_US |
dc.contributor.author | Weng, Chia-Wei | en_US |
dc.contributor.author | Tsai, Mei-Ling | en_US |
dc.contributor.author | Cheng, Ting-Jen Rachel | en_US |
dc.contributor.author | Chen, Jeremy J W | en_US |
dc.contributor.author | Lee, Te-Chang | en_US |
dc.contributor.author | Wong, Chi-Huey | en_US |
dc.contributor.author | Chein, Rong-Jie | en_US |
dc.contributor.author | PAN-CHYR YANG | en_US |
dc.date.accessioned | 2023-01-06T06:48:00Z | - |
dc.date.available | 2023-01-06T06:48:00Z | - |
dc.date.issued | 2019-11-01 | - |
dc.identifier.issn | 0223-5234 | - |
dc.identifier.uri | https://scholars.lib.ntu.edu.tw/handle/123456789/626950 | - |
dc.description.abstract | Developing new therapeutic strategies to overcome drug resistance of cancer cells is an ongoing endeavor. From among 2 million chemicals, we identified ethyl 4-oxo-2-phenyl-1,4-dihydroquinoline-6-carboxylate (AS1712) as a low-toxicity inhibitor of lung cancer cell proliferation and xenograft tumor growth. We show that AS1712 is active against broad cancer cell lines and is able to bind in the colchicine-binding pocket of β-tubulin, thereby inhibiting microtubule assembly and, consequently, inducing mitotic arrest and apoptosis. Our cell-based structure-activity relationship study identified a new lead compound, RJ-LC-15-8, which had a greater anti-proliferative potency for H1975 cells than did AS1712, while maintaining a similar mechanism of action. Notably, AS1712 and RJ-LC-15-8 overcame P-glycoprotein efflux pump and β-tubulin alterations that lead to acquired resistance against microtubule-targeting drugs of cancer cells. AS1712 and RJ-LC-15-8 may be lead compounds that overcome acquired resistance to microtubule-targeting agents of cancer cells. | en_US |
dc.language.iso | en | en_US |
dc.publisher | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | en_US |
dc.relation.ispartof | European journal of medicinal chemistry | en_US |
dc.subject | Acquired resistance; Microtubule-targeting agents; p-glycoprotein | en_US |
dc.subject.classification | [SDGs]SDG3 | - |
dc.title | 4(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin | en_US |
dc.type | journal article | en |
dc.identifier.doi | 10.1016/j.ejmech.2019.111584 | - |
dc.identifier.pmid | 31419740 | - |
dc.identifier.scopus | 2-s2.0-85070512476 | - |
dc.identifier.isi | WOS:000493211900039 | - |
dc.identifier.url | https://scholars.lib.ntu.edu.tw/handle/123456789/523434 | - |
dc.relation.journalvolume | 181 | en_US |
item.fulltext | no fulltext | - |
item.languageiso639-1 | en | - |
item.openairecristype | http://purl.org/coar/resource_type/c_6501 | - |
item.cerifentitytype | Publications | - |
item.openairetype | journal article | - |
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.orcid | 0000-0001-6330-6048 | - |
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 | - |
顯示於: | 醫學系 |
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