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Can I read Suppression of Drug-Resistant Non-Small-Cell Lung Cancer with Inhibitors Targeting Minichromosomal Maintenance Protein on EtoBox?
Suppression of Drug-Resistant Non-Small-Cell Lung Cancer with Inhibitors Targeting Minichromosomal Maintenance Protein by Chia-Yi Lin; Hsin-Yi Wu; Yuan-Ling Hsu; Ting-Jen Rachel Cheng; Jyung-Hurng Liu; Rou-Jie Huang; Tzu-Hung Hsiao; Chia-Jen Wang; Pei-Fang Hung; Albert Lan; Szu-Hua Pan; Rong-Jie Chein; Chi-Huey Wong; Pan-Chyr Yang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Suppression of Drug-Resistant Non-Small-Cell Lung Cancer with Inhibitors Targeting Minichromosomal Maintenance Protein about?
Drug resistance has been a major threat in cancer therapies that necessitates the development of new strategies to overcome this problem. We report here a cell-based high-throughput screen of a library containing two-million molecules for the compounds that inhibit the proliferation of non-small-cell lung cancer (NSCLC). Through the process of phenotypic screening, target deconvolution, and structure-activity relationship (SAR) analysis, a compound of furanonaphthoquinone-based small molecule, AS4583, was identified that exhibited potent activity in tyrosine kinase inhibitor (TKI)-sensitive and TKI-resistant NSCLC cells (IC = 77 nM) and in xenograft mice. The mechanistic studies revealed that AS4583 inhibited cell-cycle progression and reduced DNA replication by disrupting the formation of the minichromosomal maintenance protein (MCM) complex. Subsequent SAR study of AS4583 gave compound RJ-LC-07-48 which exhibited greater potency in drug-resistant NSCLC cells (IC = 17 nM) and in mice with H1975 xenograft tumor.
Who reads Suppression of Drug-Resistant Non-Small-Cell Lung Cancer with Inhibitors Targeting Minichromosomal Maintenance Protein?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Chia-Yi Lin; Hsin-Yi Wu; Yuan-Ling Hsu; Ting-Jen Rachel Cheng; Jyung-Hurng Liu; Rou-Jie Huang; Tzu-Hung Hsiao; Chia-Jen Wang; Pei-Fang Hung; Albert Lan; Szu-Hua Pan; Rong-Jie Chein; Chi-Huey Wong; Pan-Chyr Yang
- Publisher
- American Chemical Society; American Chemical Society (ACS) (ISSN 0022-2623)
- Published
- 2020
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)