使用比卡鲁胺类似物-沙利度胺PROTACs对雄激素受体（AR）进行化学降解
Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog-Thalidomide PROTACs.
作者信息
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
机构信息
College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 02447, Korea.
Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 02447, Korea.
出版信息
Molecules. 2021 Apr 26;26(9):2525. doi: 10.3390/molecules26092525.
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 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.
设计、合成并生物学评估了一系列由比卡鲁胺类似物和沙利度胺组成的PROTAC（蛋白酶靶向嵌合体），作为新型雄激素受体（AR）降解剂。特别地，我们发现PROTAC化合物能够成功地在AR阳性癌细胞中证明AR的靶向降解，并且可能是用于研究AR依赖性癌细胞的有用化学探针，以及前列腺癌的潜在治疗候选物。
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