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Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs
Technologies that induce targeted protein degradation by small molecules have been developed recently. Chimeric small molecules such as Proteolysis Targeting Chimeras (PROTACs) and Specific and Non-genetic IAP-dependent Protein Erasers (SNIPERs), and E3 modulators such as thalidomides, hijack the ce...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6914816/ https://www.ncbi.nlm.nih.gov/pubmed/31921772 http://dx.doi.org/10.3389/fchem.2019.00849 |
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author | Naito, Mikihiko Ohoka, Nobumichi Shibata, Norihito Tsukumo, Yoshinori |
author_facet | Naito, Mikihiko Ohoka, Nobumichi Shibata, Norihito Tsukumo, Yoshinori |
author_sort | Naito, Mikihiko |
collection | PubMed |
description | Technologies that induce targeted protein degradation by small molecules have been developed recently. Chimeric small molecules such as Proteolysis Targeting Chimeras (PROTACs) and Specific and Non-genetic IAP-dependent Protein Erasers (SNIPERs), and E3 modulators such as thalidomides, hijack the cellular machinery for ubiquitylation, and the ubiquitylated proteins are subjected to proteasomal degradation. This has motivated drug development in industry and academia because “undruggable targets” can now be degraded by targeted protein degradation. |
format | Online Article Text |
id | pubmed-6914816 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-69148162020-01-09 Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs Naito, Mikihiko Ohoka, Nobumichi Shibata, Norihito Tsukumo, Yoshinori Front Chem Chemistry Technologies that induce targeted protein degradation by small molecules have been developed recently. Chimeric small molecules such as Proteolysis Targeting Chimeras (PROTACs) and Specific and Non-genetic IAP-dependent Protein Erasers (SNIPERs), and E3 modulators such as thalidomides, hijack the cellular machinery for ubiquitylation, and the ubiquitylated proteins are subjected to proteasomal degradation. This has motivated drug development in industry and academia because “undruggable targets” can now be degraded by targeted protein degradation. Frontiers Media S.A. 2019-12-10 /pmc/articles/PMC6914816/ /pubmed/31921772 http://dx.doi.org/10.3389/fchem.2019.00849 Text en Copyright © 2019 Naito, Ohoka, Shibata and Tsukumo. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Chemistry Naito, Mikihiko Ohoka, Nobumichi Shibata, Norihito Tsukumo, Yoshinori Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs |
title | Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs |
title_full | Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs |
title_fullStr | Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs |
title_full_unstemmed | Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs |
title_short | Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs |
title_sort | targeted protein degradation by chimeric small molecules, protacs and snipers |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6914816/ https://www.ncbi.nlm.nih.gov/pubmed/31921772 http://dx.doi.org/10.3389/fchem.2019.00849 |
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