TACkling Cancer by Targeting Selective Protein Degradation
Targeted protein degradation has emerged as an alternative therapy against cancer, offering several advantages over traditional inhibitors. The new degrader drugs provide different therapeutic strategies: they could cross the phospholipid bilayer membrane by the addition of specific moieties to extr...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-10-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/10/2442 |
| _version_ | 1797572546986508288 |
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| author | María del Mar Noblejas-López David Tébar-García Raquel López-Rosa Ana Alcaraz-Sanabria Pablo Cristóbal-Cueto Alejandro Pinedo-Serrano Lorenzo Rivas-García Eva M. Galán-Moya |
| author_facet | María del Mar Noblejas-López David Tébar-García Raquel López-Rosa Ana Alcaraz-Sanabria Pablo Cristóbal-Cueto Alejandro Pinedo-Serrano Lorenzo Rivas-García Eva M. Galán-Moya |
| author_sort | María del Mar Noblejas-López |
| collection | DOAJ |
| description | Targeted protein degradation has emerged as an alternative therapy against cancer, offering several advantages over traditional inhibitors. The new degrader drugs provide different therapeutic strategies: they could cross the phospholipid bilayer membrane by the addition of specific moieties to extracellular proteins. On the other hand, they could efficiently improve the degradation process by the generation of a ternary complex structure of an E3 ligase. Herein, we review the current trends in the use of TAC-based technologies (TACnologies), such as PROteolysis TArgeting Chimeras (PROTAC), PHOtochemically TArgeting Chimeras (PHOTAC), CLIck-formed Proteolysis TArgeting Chimeras (CLIPTAC), AUtophagy TArgeting Chimeras (AUTAC), AuTophagosome TEthering Compounds (ATTEC), LYsosome-TArgeting Chimeras (LYTAC), and DeUBiquitinase TArgeting Chimeras (DUBTAC), in experimental development and their progress towards clinical applications. |
| first_indexed | 2024-03-10T20:58:24Z |
| format | Article |
| id | doaj.art-25899f23c6a746d5995a9daa49ed80ef |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T20:58:24Z |
| publishDate | 2023-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-25899f23c6a746d5995a9daa49ed80ef2023-11-19T17:44:34ZengMDPI AGPharmaceutics1999-49232023-10-011510244210.3390/pharmaceutics15102442TACkling Cancer by Targeting Selective Protein DegradationMaría del Mar Noblejas-López0David Tébar-García1Raquel López-Rosa2Ana Alcaraz-Sanabria3Pablo Cristóbal-Cueto4Alejandro Pinedo-Serrano5Lorenzo Rivas-García6Eva M. Galán-Moya7Centro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainCentro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainCentro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainCentro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainCentro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainCentro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainCentro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainCentro Regional de Investigaciones Biomédicas (CRIB), Campus de Albacete, Universidad de Castilla-La Mancha, 02008 Albacete, SpainTargeted protein degradation has emerged as an alternative therapy against cancer, offering several advantages over traditional inhibitors. The new degrader drugs provide different therapeutic strategies: they could cross the phospholipid bilayer membrane by the addition of specific moieties to extracellular proteins. On the other hand, they could efficiently improve the degradation process by the generation of a ternary complex structure of an E3 ligase. Herein, we review the current trends in the use of TAC-based technologies (TACnologies), such as PROteolysis TArgeting Chimeras (PROTAC), PHOtochemically TArgeting Chimeras (PHOTAC), CLIck-formed Proteolysis TArgeting Chimeras (CLIPTAC), AUtophagy TArgeting Chimeras (AUTAC), AuTophagosome TEthering Compounds (ATTEC), LYsosome-TArgeting Chimeras (LYTAC), and DeUBiquitinase TArgeting Chimeras (DUBTAC), in experimental development and their progress towards clinical applications.https://www.mdpi.com/1999-4923/15/10/2442protein degraderPROTACPHOTACCLIPTACAUTACATTEC |
| spellingShingle | María del Mar Noblejas-López David Tébar-García Raquel López-Rosa Ana Alcaraz-Sanabria Pablo Cristóbal-Cueto Alejandro Pinedo-Serrano Lorenzo Rivas-García Eva M. Galán-Moya TACkling Cancer by Targeting Selective Protein Degradation Pharmaceutics protein degrader PROTAC PHOTAC CLIPTAC AUTAC ATTEC |
| title | TACkling Cancer by Targeting Selective Protein Degradation |
| title_full | TACkling Cancer by Targeting Selective Protein Degradation |
| title_fullStr | TACkling Cancer by Targeting Selective Protein Degradation |
| title_full_unstemmed | TACkling Cancer by Targeting Selective Protein Degradation |
| title_short | TACkling Cancer by Targeting Selective Protein Degradation |
| title_sort | tackling cancer by targeting selective protein degradation |
| topic | protein degrader PROTAC PHOTAC CLIPTAC AUTAC ATTEC |
| url | https://www.mdpi.com/1999-4923/15/10/2442 |
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