Author:
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
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.
Funder
National Research Foundation of Korea
Subject
Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science
Cited by
23 articles.
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