PROTAC: targeted drug strategy. Principles and limitations

The PROTAC (PROteolysis TArgeting Chimera) technology is a method of targeting intracellular proteins previously considered undruggable. This technology utilizes the ubiquitin—proteasome system in cells to specifically degrade target proteins, thereby offering significant advantages over conventiona...

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Autores principales: Koroleva, O. A., Dutikova, Yu. V., Trubnikov, A. V., Zenov, F. A., Manasova, E. V., Shtil, A. A., Kurkin, A. V.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2022
Materias:
Reviews
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9762658/
https://www.ncbi.nlm.nih.gov/pubmed/36569659
http://dx.doi.org/10.1007/s11172-022-3659-z
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author Koroleva, O. A.
Dutikova, Yu. V.
Trubnikov, A. V.
Zenov, F. A.
Manasova, E. V.
Shtil, A. A.
Kurkin, A. V.
author_facet Koroleva, O. A.
Dutikova, Yu. V.
Trubnikov, A. V.
Zenov, F. A.
Manasova, E. V.
Shtil, A. A.
Kurkin, A. V.
author_sort Koroleva, O. A.
collection PubMed
description The PROTAC (PROteolysis TArgeting Chimera) technology is a method of targeting intracellular proteins previously considered undruggable. This technology utilizes the ubiquitin—proteasome system in cells to specifically degrade target proteins, thereby offering significant advantages over conventional small-molecule inhibitors of the enzymatic function. Preclinical and preliminary clinical trials of PROTAC-based compounds (degraders) are presented. The review considers the general principles of the design of degraders. Advances and challenges of the PROTAC technology are discussed.
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spelling pubmed-97626582022-12-20 PROTAC: targeted drug strategy. Principles and limitations Koroleva, O. A. Dutikova, Yu. V. Trubnikov, A. V. Zenov, F. A. Manasova, E. V. Shtil, A. A. Kurkin, A. V. Russ Chem Bull Reviews The PROTAC (PROteolysis TArgeting Chimera) technology is a method of targeting intracellular proteins previously considered undruggable. This technology utilizes the ubiquitin—proteasome system in cells to specifically degrade target proteins, thereby offering significant advantages over conventional small-molecule inhibitors of the enzymatic function. Preclinical and preliminary clinical trials of PROTAC-based compounds (degraders) are presented. The review considers the general principles of the design of degraders. Advances and challenges of the PROTAC technology are discussed. Springer US 2022-12-19 2022 /pmc/articles/PMC9762658/ /pubmed/36569659 http://dx.doi.org/10.1007/s11172-022-3659-z Text en © Springer Science+Business Media LLC 2022 This article is made available via the PMC Open Access Subset for unrestricted research re-use and secondary analysis in any form or by any means with acknowledgement of the original source. These permissions are granted for the duration of the World Health Organization (WHO) declaration of COVID-19 as a global pandemic.
spellingShingle Reviews
Koroleva, O. A.
Dutikova, Yu. V.
Trubnikov, A. V.
Zenov, F. A.
Manasova, E. V.
Shtil, A. A.
Kurkin, A. V.
PROTAC: targeted drug strategy. Principles and limitations
title PROTAC: targeted drug strategy. Principles and limitations
title_full PROTAC: targeted drug strategy. Principles and limitations
title_fullStr PROTAC: targeted drug strategy. Principles and limitations
title_full_unstemmed PROTAC: targeted drug strategy. Principles and limitations
title_short PROTAC: targeted drug strategy. Principles and limitations
title_sort protac: targeted drug strategy. principles and limitations
topic Reviews
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9762658/
https://www.ncbi.nlm.nih.gov/pubmed/36569659
http://dx.doi.org/10.1007/s11172-022-3659-z
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