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

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 degrad...

Descripción completa

Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8123623/
https://www.ncbi.nlm.nih.gov/pubmed/33926033
http://dx.doi.org/10.3390/molecules26092525
Descripción
Sumario: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.

Ejemplares similares