Research progress in controllable proteolysis targeting chimeras / 药学学报
Acta Pharmaceutica Sinica
;
(12): 2193-2202, 2023.
Artigo
em Chinês
| WPRIM
| ID: wpr-999149
ABSTRACT
Proteolysis targeting chimeras (PROTACs) is an innovative technique in targeted protein degradation. PROTACs is a heterobifunctional molecule which can bind to the E3 ligase and target protein to form a ubiquitination complex, resulting in the ubiquitin-proteasome system dependent degradation of target protein. PROTACs has been regarded as the promising method in drug discovery campaign, for its high commonality, potent degradation activity and unique selectivity profile. However, the catalytic mechanism also induces the uncontrollable protein degradation risk. Controllable PROTACs contain the responsive element in the molecular entity. In certain conditions, the element can be triggered to activate or terminate the degradation event. In this review, we will briefly summarize the strategies in controllable PROTACs and describe the representative examples according to the responsive mechanism. We hope this review could provide some insight into the further development of controllable PROTACs.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2023
Tipo de documento:
Artigo
Similares
MEDLINE
...
LILACS
LIS