Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity
- Authors
- Kim, Yong-Hak; Ha, Siyoung; Kim, Jungwon; Ham, Seung Wook
- Issue Date
- Jul-2016
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- anticancer agents; competitive binding; KPNB1; LC-MS; MS; proteomics
- Citation
- CHEMMEDCHEM, v.11, no.13, pp 1406 - 1409
- Pages
- 4
- Journal Title
- CHEMMEDCHEM
- Volume
- 11
- Number
- 13
- Start Page
- 1406
- End Page
- 1409
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/6742
- DOI
- 10.1002/cmdc.201600159
- ISSN
- 1860-7179
1860-7187
- Abstract
- We found that aminothiazole derivative (E)-N-(5-benzylthiazol-2-yl)-3-(furan-2-yl)acrylamide (1) has strong anticancer activity, and undertook proteomics approaches to identify the target protein of compound 1, importin1 (KPNB1). A competitive binding assay using fluorescein-labeled 1 showed that 1 has strong binding affinity for KPNB1 (K-d: approximate to 20nm). Furthermore, through western blotting assays for KPNB1, KPNA2, EGFR, ErbB2, and STAT3, we confirmed that 1 has inhibitory effects on the importin pathway. KPBN1 appears to be overexpressed in several cancer cells, and siRNA-induced inhibition of KPNB1 shows significant inhibition of cancer cell proliferation, while leaving non-cancerous cells unaffected. Therefore, compound 1 is a promising new lead for the development of KPNB1-targeted anticancer agents. Fluorescein-labeled 1 could be a useful quantitative probe for the development of novel KPNB1 inhibitors.
- 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
![qrcode](https://api.qrserver.com/v1/create-qr-code/?size=55x55&data=https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/6742)
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.