Advances and perspectives of proteolysis targeting chimeras (PROTACs) in drug discovery.
Bioorg Chem
; 125: 105848, 2022 08.
Article
em En
| MEDLINE
| ID: mdl-35533582
ABSTRACT
Proteolysis-targeting chimeras (PROTACs), bifunctional molecules consisting of a ligand of protein of interest (POI), an E3 ligase ligand and a linker, have been developed to hijack the ubiquitin-proteasome system (UPS) to induce different POIs degradation. Currently, the first oral PROTACs (ARV-110 and ARV-471) have shown encouraging efficacy in clinical trials of prostate and breast cancer treatment, which turns a new avenue for the development of PROTAC research. In this review, we focus on a detailed summary of the latest progress of PROTACs and elucidate the advantages of PROTACs technology. In addition, potential challenges and perspectives of PRTOACs are discussed.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Ubiquitina-Proteína Ligases
/
Descoberta de Drogas
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Proteólise
Idioma:
En
Revista:
Bioorg Chem
Ano de publicação:
2022
Tipo de documento:
Article
País de afiliação:
China