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

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...

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Detalles Bibliográficos
Autores principales: Luo, Guoshun, Li, Zhenbang, Lin, Xin, Li, Xinyu, Chen, Yu, Xi, Kun, Xiao, Maoxu, Wei, Hanlin, Zhu, Lizhe, Xiang, Hua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8148065/
https://www.ncbi.nlm.nih.gov/pubmed/34094835
http://dx.doi.org/10.1016/j.apsb.2020.11.001

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8148065/
https://www.ncbi.nlm.nih.gov/pubmed/34094835
http://dx.doi.org/10.1016/j.apsb.2020.11.001

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