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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 English | WPRIM | ID: wpr-881200
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 (

Full text: Available Index: WPRIM (Western Pacific) Language: English Journal: Acta Pharmaceutica Sinica B Year: 2021 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Language: English Journal: Acta Pharmaceutica Sinica B Year: 2021 Type: Article