Light-Controllable PROTACs for Temporospatial Control of Protein Degradation
PROteolysis-TArgeting Chimeras (PROTACs) is an emerging and promising approach to target intracellular proteins for ubiquitination-mediated degradation, including those so-called undruggable protein targets, such as transcriptional factors and scaffold proteins. To date, plenty of PROTACs have been...
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Frontiers Media S.A.
2021-07-01
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Series: | Frontiers in Cell and Developmental Biology |
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Online Access: | https://www.frontiersin.org/articles/10.3389/fcell.2021.678077/full |
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author | Jing Liu Yunhua Peng Wenyi Wei |
author_facet | Jing Liu Yunhua Peng Wenyi Wei |
author_sort | Jing Liu |
collection | DOAJ |
description | PROteolysis-TArgeting Chimeras (PROTACs) is an emerging and promising approach to target intracellular proteins for ubiquitination-mediated degradation, including those so-called undruggable protein targets, such as transcriptional factors and scaffold proteins. To date, plenty of PROTACs have been developed to degrade various disease-relevant proteins, such as estrogen receptor (ER), androgen receptor (AR), RTK, and CDKs. However, the on-target off-tissue and off-target effect is one of the major limitation that prevents the usage of PROTACs in clinic. To this end, we and several other groups have recently developed light-controllable PROTACs, as the representative for the third generation controllable PROTACs, by using either photo-caging or photo-switch approaches. In this review, we summarize the emerging light-controllable PROTACs and the prospective for other potential ways to achieve temporospatial control of PROTACs. |
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format | Article |
id | doaj.art-84e3097929e34b0a8dd4f6a7889f06dd |
institution | Directory Open Access Journal |
issn | 2296-634X |
language | English |
last_indexed | 2024-12-18T02:21:11Z |
publishDate | 2021-07-01 |
publisher | Frontiers Media S.A. |
record_format | Article |
series | Frontiers in Cell and Developmental Biology |
spelling | doaj.art-84e3097929e34b0a8dd4f6a7889f06dd2022-12-21T21:24:11ZengFrontiers Media S.A.Frontiers in Cell and Developmental Biology2296-634X2021-07-01910.3389/fcell.2021.678077678077Light-Controllable PROTACs for Temporospatial Control of Protein DegradationJing LiuYunhua PengWenyi WeiPROteolysis-TArgeting Chimeras (PROTACs) is an emerging and promising approach to target intracellular proteins for ubiquitination-mediated degradation, including those so-called undruggable protein targets, such as transcriptional factors and scaffold proteins. To date, plenty of PROTACs have been developed to degrade various disease-relevant proteins, such as estrogen receptor (ER), androgen receptor (AR), RTK, and CDKs. However, the on-target off-tissue and off-target effect is one of the major limitation that prevents the usage of PROTACs in clinic. To this end, we and several other groups have recently developed light-controllable PROTACs, as the representative for the third generation controllable PROTACs, by using either photo-caging or photo-switch approaches. In this review, we summarize the emerging light-controllable PROTACs and the prospective for other potential ways to achieve temporospatial control of PROTACs.https://www.frontiersin.org/articles/10.3389/fcell.2021.678077/fullubiquitinE3 ligasePROTACtumorigenesislight controllable |
spellingShingle | Jing Liu Yunhua Peng Wenyi Wei Light-Controllable PROTACs for Temporospatial Control of Protein Degradation Frontiers in Cell and Developmental Biology ubiquitin E3 ligase PROTAC tumorigenesis light controllable |
title | Light-Controllable PROTACs for Temporospatial Control of Protein Degradation |
title_full | Light-Controllable PROTACs for Temporospatial Control of Protein Degradation |
title_fullStr | Light-Controllable PROTACs for Temporospatial Control of Protein Degradation |
title_full_unstemmed | Light-Controllable PROTACs for Temporospatial Control of Protein Degradation |
title_short | Light-Controllable PROTACs for Temporospatial Control of Protein Degradation |
title_sort | light controllable protacs for temporospatial control of protein degradation |
topic | ubiquitin E3 ligase PROTAC tumorigenesis light controllable |
url | https://www.frontiersin.org/articles/10.3389/fcell.2021.678077/full |
work_keys_str_mv | AT jingliu lightcontrollableprotacsfortemporospatialcontrolofproteindegradation AT yunhuapeng lightcontrollableprotacsfortemporospatialcontrolofproteindegradation AT wenyiwei lightcontrollableprotacsfortemporospatialcontrolofproteindegradation |