Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity
Acta Pharmaceutica Sinica B
; (6): 1300-1314, 2021.
Article
em En
| WPRIM
| ID: wpr-881200
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WPRO
ABSTRACT
HMG-CoA reductase (HMGCR) protein is usually upregulated after statin (HMGCR inhibitor) treatment, which inevitably diminishes its therapeutic efficacy, provoking the need for higher doses associated with adverse effects. The proteolysis targeting chimera (PROTAC) technology has recently emerged as a powerful approach for inducing protein degradation. Nonetheless, due to their bifunctional nature, developing orally bioavailable PROTACs remains a great challenge. Herein, we identified a powerful HMGCR-targeted PROTAC (
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WPRIM
Idioma:
En
Revista:
Acta Pharmaceutica Sinica B
Ano de publicação:
2021
Tipo de documento:
Article