Chimera induced protein degradation: PROTACs and beyond.
Eur J Med Chem
; 206: 112494, 2020 Nov 15.
Article
en En
| MEDLINE
| ID: mdl-32890974
Ubiquitin-proteasome system, autophagy-lysosome pathway and N-end rule pathway are crucial protein quality control mechanisms in human body. Hijacking these endogenous protein degrading measures by chimera degraders could be a revolutionary strategy for the discovery of small-molecule drugs. As the most advanced chimera degraders, PROTACs have demonstrated the potential by delivering two drug candidates into clinical trials. The development of chimera degraders exploiting these three pathways are reviewed, a focus is given on the chemical structures and their influences on biological effects from a viewpoint of medicinal chemistry.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Ubiquitina
/
Complejo de la Endopetidasa Proteasomal
/
Descubrimiento de Drogas
/
Proteolisis
Límite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Año:
2020
Tipo del documento:
Article
Pais de publicación:
Francia