Detailed Information
Cited 1 time in 
Cited 1 time in 
Cited 1 time in
Metadata Downloads
Determination of the binding site of 2-aminothiazole derivative with importin beta 1 by UV-crosslinking experiment
- Authors
- Ha, Siyoung; Oh, Jiwon; Kim, Yong-Hak; Ham, Seung Wook
- Issue Date
- Aug-2017
- Publisher
- ELSEVIER SCIENCE BV
- Citation
- JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, v.1060, pp 71 - 75
- Pages
- 5
- Journal Title
- JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
- Volume
- 1060
- Start Page
- 71
- End Page
- 75
- ISSN
- 1570-0232
1873-376X
- Abstract
- Importin beta 1 (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.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - College of Natural Sciences > Department of Chemistry > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.