Progress of small molecules for targeted protein degradation: PROTACs and other technologies.
Drug Dev Res
; 84(2): 337-394, 2023 04.
Article
em En
| MEDLINE
| ID: mdl-36606428
ABSTRACT
Recent years have witnessed the rapid development of targeted protein degradation (TPD), especially proteolysis targeting chimeras. These degraders have manifested many advantages over small molecule inhibitors. To date, a huge number of degraders have been excavated against over 70 disease-related targets. In particular, degraders against estrogen receptor and androgen receptor have crowded into phase II clinical trial. TPD technologies largely expand the scope of druggable targets, and provide powerful tools for addressing intractable problems that can not be tackled by traditional small molecule inhibitors. In this review, we mainly focus on the structures and biological activities of small molecule degraders as well as the elucidation of mechanisms of emerging TPD technologies. We also propose the challenges that exist in the TPD field at present.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores de Estrogênio
/
Quimera de Direcionamento de Proteólise
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article