Homo-PROTAC mediated suicide of MDM2 to treat non-small cell lung cancer
Acta Pharmaceutica Sinica B
; (6): 1617-1628, 2021.
Article
em En
| WPRIM
| ID: wpr-888824
Biblioteca responsável:
WPRO
ABSTRACT
The dose-related adverse effects of MDM2‒P53 inhibitors have caused significant concern in the development of clinical safe anticancer agents. Herein we report an unprecedented homo-PROTAC strategy for more effective disruption of MDM2‒P53 interaction. The design concept is inspired by the capacity of sub-stoichiometric catalytic PROTACs enabling to degrade an unwanted protein and the dual functions of MDM2 as an E3 ubiquitin ligase and a binding protein with tumor suppressor P53. The new homo-PROTACs are designed to induce self-degradation of MDM2. The results of the investigation have shown that PROTAC
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Índice:
WPRIM
Idioma:
En
Revista:
Acta Pharmaceutica Sinica B
Ano de publicação:
2021
Tipo de documento:
Article