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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...
Autores principales: | Luo, Guoshun, Li, Zhenbang, Lin, Xin, Li, Xinyu, Chen, Yu, Xi, Kun, Xiao, Maoxu, Wei, Hanlin, Zhu, Lizhe, Xiang, Hua |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2021
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Materias: | |
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 |
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