國家衛生研究院 NHRI:Item 3990099045/6211
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    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/6211


    Title: A High-throughput cell-based screening for L858R/T790M mutant epidermal growth factor receptor inhibitors
    Authors: Lin, WH;Song, JS;Lien, TW;Chang, CY;Wu, SH;Huang, YW;Chang, TY;Fang, MY;Yen, KJ;Chen, CH;Chu, CY;Hsieh, HP;Chen, YR;Chao, YS;Hsu, JT
    Contributors: Institute of Biotechnology and Pharmaceutical Research;Institute of Molecular and Genomic Medicine
    Abstract: A high-throughput 32D(L858R/T790M) cell-based assay to identify inhibitors of the L858R/T790M mutant epidermal growth factor receptor (EGFR) pathway was established. After screening, ten hits from among 60,000 compounds in our in-house compound library were initially identified. In the secondary assays, one hit, 1-[2-(decyloxy)-2-oxoethyl]-3-methyl-2-[(4-methylphenoxy) methyl]-1H-benzimidazol-3-ium, was confirmed to directly inhibit the kinase activity of recombinant L858R/T790M EGFR and the phosphorylation of EGFR-L858R/T790M in gefitinib-resistant H1975 cells. Thus, this high-throughput assay system may be useful for identifying novel inhibitors which suppress mutant EGFR-T790M signalling and for overcoming T790M-mediated acquired resistance for future anticancer drug discovery.
    Date: 2012-01
    Relation: Anticancer Research. 2012 Jan;32(1):147-151.
    Link to: http://ar.iiarjournals.org/content/32/1/147.abstract
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0250-7005&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000298780900019
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84862937281
    Appears in Collections:[John Tsu-An Hsu] Periodical Articles
    [Yu-Sheng Chao(2002-2013)] Periodical Articles
    [Hsing-Pang Hsieh] Periodical Articles
    [Yi-Rong Chen] Periodical Articles

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