Discovery of MD-224 as a First-in-Class, Highly Potent and Efficacious PROTAC MDM2 Degrader Capable of Achieving Complete and Durable Tumor Regression

Human murine double minute 2 (MDM2) protein is a primary endogenous cellular inhibitor of the tumor suppressor p53 and has been pursued as an attractive cancer therapeutic target. Several potent, non-peptide small-molecule inhibitors of MDM2 are currently in clinical development. In this paper, we r...

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Pubblicato in:J Med Chem
Autori principali: Li, Yangbing, Yang, Jiuling, Aguilar, Angelo, McEachern, Donna, Przybranowski, Sally, Liu, Liu, Yang, Chao-Yie, Wang, Mi, Han, Xin, Wang, Shaomeng
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2018
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC6545112/
https://ncbi.nlm.nih.gov/pubmed/30525597
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00909
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