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Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders

The aberrant expression of protein arginine methyltransferase 5 (PRMT5) has been associated with multiple cancers. Using the proteolysis targeting chimera technology, we discovered a first-in-class PRMT5 degrader 15 (MS4322). Here, we report the design, synthesis, and characterization of compound 15...

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Bibliographische Detailangaben
Veröffentlicht in:J Med Chem
Hauptverfasser: Shen, Yudao, Gao, Guozhen, Yu, Xufen, Kim, Huensuk, Wang, Li, Xie, Ling, Schwarz, Megan, Chen, Xian, Guccione, Ernesto, Liu, Jing, Bedford, Mark T., Jin, Jian
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2020
Schlagworte:
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7486226/
https://ncbi.nlm.nih.gov/pubmed/32787082
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c01111
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