Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

Current efforts in the proteolysis targeting chimera (PROTAC) field mostly focus on choosing an appropriate E3 ligase for the target protein, improving the binding affinities towards the target protein and the E3 ligase, and optimizing the PROTAC linker. However, due to the large molecular weights o...

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Pubblicato in:Nat Commun
Autori principali: Guo, Wen-Hao, Qi, Xiaoli, Yu, Xin, Liu, Yang, Chung, Chan-I, Bai, Fang, Lin, Xingcheng, Lu, Dong, Wang, Lingfei, Chen, Jianwei, Su, Lynn Hsiao, Nomie, Krystle J., Li, Feng, Wang, Meng C., Shu, Xiaokun, Onuchic, José N., Woyach, Jennifer A., Wang, Michael L., Wang, Jin
Natura: Artigo
Lingua:Inglês
Pubblicazione: Nature Publishing Group UK 2020
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC7450057/
https://ncbi.nlm.nih.gov/pubmed/32848159
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41467-020-17997-6
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