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...

Descripción completa

Detalles Bibliográficos
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
Descripción
Sumario: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.

Ejemplares similares