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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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7450057/
https://www.ncbi.nlm.nih.gov/pubmed/32848159
http://dx.doi.org/10.1038/s41467-020-17997-6

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