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. 2022 Dec 19;71(11):2310–2334. doi: 10.1007/s11172-022-3659-z

PROTAC: targeted drug strategy. Principles and limitations

O A Koroleva 1, Yu V Dutikova 2, A V Trubnikov 1, F A Zenov 1, E V Manasova 1, A A Shtil 1,3, A V Kurkin 1,✉
PMCID: PMC9762658  PMID: 36569659

Abstract

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.

Key words: PROTAC technology, proteolysis, cancer therapy

Footnotes

Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 11, pp. 2310–2334, November, 2022.

The work was financially supported by the Russian Foundation for Basic Research (Project No. 20-53-7808 Ital_t).

No human or animal subjects were used in this research.

The authors declare no competing interests.

Contributor Information

Yu. V. Dutikova, Email: Dutikova@azalesov.com

A. A. Shtil, Email: shtilaa@yahoo.com

A. V. Kurkin, Email: indolester@gmail.com

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