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- Title
Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs.
- Authors
Kim, Ga Yeong; Song, Chae Won; Yang, Yo-Sep; Lee, Na-Rae; Yoo, Hyung-Seok; Son, Seung Hwan; Lee, Soo Jin; Park, Jong Seon; Lee, Jong Kil; Inn, Kyung-Soo; Kim, Nam-Jung; Hodgkinson, James T.
- Abstract
A series of PROTACs (PROteolysis-TArgeting Chimeras) consisting of bicalutamide analogs and thalidomides were designed, synthesized, and biologically evaluated as novel androgen receptor (AR) degraders. In particular, we found that PROTAC compound 13b could successfully demonstrate a targeted degradation of AR in AR-positive cancer cells and might be a useful chemical probe for the investigation of AR-dependent cancer cells, as well as a potential therapeutic candidate for prostate cancers.
- Subjects
ANDROGEN receptors; CHEMICAL decomposition; CANCER cells; PROSTATE cancer; PROTEOLYSIS
- Publication
Molecules, 2021, Vol 26, Issue 9, p2525
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26092525