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
in En
| WPRIM
| ID: wpr-881200
Responsible library:
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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Language:
En
Journal:
Acta Pharmaceutica Sinica B
Year:
2021
Type:
Article