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

Autor:	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
Jazyk:	angličtina
Rok vydání:	2021
Předmět:	bicalutamide protein degradation PROTAC androgen receptor (AR) prostate cancer Organic chemistry QD241-441
Zdroj:	Molecules, Vol 26, Iss 9, p 2525 (2021)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules26092525
Popis:	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.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/32dd86b792cc47b8baed18485d0d87de Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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