상세 보기
Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog-Thalidomide PROTACs
- Kim, Ga Yeong;
- Song, Chae Won;
- Yang, Yo-Sep;
- Lee, Na-Rae;
- Yoo, Hyung-Seok;
- ... Son, Seung Hwan;
- 외 5명
Citations
WEB OF SCIENCE
28Citations
SCOPUS
34초록
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.
키워드
bicalutamide; protein degradation; PROTAC; androgen receptor (AR); prostate cancer; PROSTATE; RESISTANCE; DESIGN
- 제목
- Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog-Thalidomide PROTACs
- 저자
- 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
- 발행일
- 2021-05
- 유형
- Article
- 저널명
- Molecules
- 권
- 26
- 호
- 9
- 언어
- ENG
- 출판사
- MDPI
- 발행국가
- 스위스
- ISSN
- E 1420-3049