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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...
| Autores principales: | , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2021
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| Materias: | |
| 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 |
| _version_ | 1783692961113964544 |
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| 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 |
| author_facet | 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 |
| author_sort | Kim, Ga Yeong |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-8123623 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2021 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-81236232021-05-16 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 Lee, Soo Jin Park, Jong Seon Lee, Jong Kil Inn, Kyung-Soo Kim, Nam-Jung Molecules Article 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. MDPI 2021-04-26 /pmc/articles/PMC8123623/ /pubmed/33926033 http://dx.doi.org/10.3390/molecules26092525 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
| spellingShingle | Article 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 Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs |
| title | Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs |
| title_full | Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs |
| title_fullStr | Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs |
| title_full_unstemmed | Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs |
| title_short | Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog–Thalidomide PROTACs |
| title_sort | chemical degradation of androgen receptor (ar) using bicalutamide analog–thalidomide protacs |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8123623/ https://www.ncbi.nlm.nih.gov/pubmed/33926033 http://dx.doi.org/10.3390/molecules26092525 |
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