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

• Автори: Guoshun Luo (Автор), Zhenbang Li (Автор), Xin Lin (Автор), Xinyu Li (Автор), Yu Chen (Автор), Kun Xi (Автор), Maoxu Xiao (Автор), Hanlin Wei (Автор), Lizhe Zhu (Автор), Hua Xiang (Автор)
• Формат: Книга
• Опубліковано: Elsevier, 2021-05-01T00:00:00Z.
• Предмети: article
• Онлайн доступ: 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...