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Article

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

Nature communications - 26 Aug 2020

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

Abstract excerpt

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 of PROTACs, their cellular uptake remains an issue. Through comparing how different warhead chemistry, reversible...

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Identifiers

PMID: 32848159
DOI: 10.1038/s41467-020-17997-6
PMCID: PMC7450057

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