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Proteolysis targeting chimeras (PROTACs) in cancer therapy.

ABSTRACT: Exploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs). PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ligase. The bridging between the protein of interest and the E3 ligase mediated by the PROTAC facilitates ubiquitination of the protein and its proteasomal degradation. In this review we discuss the molecular medicine behind PROTAC mechanism of action, with special emphasis on recent developments and their potential translation to the clinical setting.

SUBMITTER: Ocana A

PROVIDER: S-EPMC7493969 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature

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Proteolysis targeting chimeras (PROTACs) in cancer therapy.

Ocaña Alberto A Pandiella Atanasio A

Journal of experimental & clinical cancer research : CR 20200915 1

Exploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs). PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ligase. The bridging between the protein of interest and the E3 ligase mediated by the PROTAC facilitates ubiquitination of the protein and its proteasomal ...[more]

PMID: 32933565

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| S-EPMC8190915 | biostudies-literature

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