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Simple Structural Modifications Converting a Bona Fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders

Inducing protein degradation by proteolysis targeting chimeras (PROTACs) has gained tremendous momentum for its promise to discover and develop new therapies. Based upon our previously reported PROTAC MDM2 degraders, we have designed and synthesized additional analogues. Surprisingly, we found that...

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Опубликовано в: :J Med Chem
Главные авторы: Yang, Jiuling, Li, Yangbing, Aguilar, Angelo, Liu, Zhaomin, Yang, Chao-Yie, Wang, Shaomeng
Формат: Artigo
Язык:Inglês
Опубликовано: 2019
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Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC7354697/
https://ncbi.nlm.nih.gov/pubmed/31560543
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b00846
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