Progress in RAS-targeted therapeutic strategies: From small molecule inhibitors to proteolysis targeting chimeras.
Med Res Rev
; 44(2): 812-832, 2024 Mar.
Article
en En
| MEDLINE
| ID: mdl-38009264
ABSTRACT
As a widely considerable target in chemical biology and pharmacological research, rat sarcoma (RAS) gene mutations play a critical driving factor in several fatal cancers. Despite the great progress of RAS subtype-specific inhibitors, rapid acquired drug resistance could limit their further clinical applications. Proteolysis targeting chimera (PROTAC) has emerged as a powerful tool to handle "undruggable" targets and exhibited significant therapeutic benefit for the combat of drug resistance. Owing to unique molecular mechanism and binding kinetics, PROTAC is expected to become a feasible strategy to break the bottleneck of classical RAS inhibitors. This review aims to discuss the current advances of RAS inhibitors and especially focus on PROTAC strategy targeting RAS mutations and their downstream effectors for relevant cancer treatment.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Quimera Dirigida a la Proteólisis
Límite:
Humans
Idioma:
En
Año:
2024
Tipo del documento:
Article