Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog-Thalidomide PROTACs.

Ga-Yeong Kim, Chae Won Song, Yo-Sep Yang, Na-Rae Lee, Hyung-Seok Yoo, Seung Hwan Son, Soo Jin Lee, Jong Seon Park, Jong Kil Lee, Kyung-Soo Inn, Nam-Jung Kim

Molecules (Basel, Switzerland) 2021 Apr 26

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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.

Citation

Ga-Yeong Kim, Chae Won Song, Yo-Sep Yang, Na-Rae Lee, Hyung-Seok Yoo, Seung Hwan Son, Soo Jin Lee, Jong Seon Park, Jong Kil Lee, Kyung-Soo Inn, Nam-Jung Kim. Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog-Thalidomide PROTACs. Molecules (Basel, Switzerland). 2021 Apr 26;26(9)