Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

• Main Authors: Guoshun Luo (Author), Zhenbang Li (Author), Xin Lin (Author), Xinyu Li (Author), Yu Chen (Author), Kun Xi (Author), Maoxu Xiao (Author), Hanlin Wei (Author), Lizhe Zhu (Author), Hua Xiang (Author)
• Format: Book
• Published: Elsevier, 2021-05-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...