| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5136438 | Journal of Chromatography B | 2017 | 5 Pages |
Abstract
Importin β1 (KPBN1) appears to be overexpressed in several cancer cells and siRNA-induced inhibition of KPNB1 shows significant inhibition of cancer cell proliferation, but do not affect normal cells. These results indicate that KPNB1 is a potential target and inhibition of KPNB1 can be used as a novel therapeutic approach for the treatment of cancer. Recently, we identified the aminothiazole derivative 1 as a KPNB1-targeted anticancer agent. Herein, we report that compound 1 binds strongly to KPNB1, in a pocket centered around serine-476, as shown by UV-crosslinking and tandem mass spectrometry experiments, and supported using a model derived from molecular docking.
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Authors
Siyoung Ha, Jiwon Oh, Yong-Hak Kim, Seung Wook Ham,