Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
PROTACs have emerged as promising therapeutic agents but their cellular uptake is often inefficient. Here, the authors show that reversible covalent warhead chemistry improves PROTAC intracellular accumulation and target engagement, and develop a dual inhibitor/degrader of Bruton’s tyrosine kinase
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Autores principales: | Wen-Hao Guo, Xiaoli Qi, Xin Yu, Yang Liu, Chan-I Chung, Fang Bai, Xingcheng Lin, Dong Lu, Lingfei Wang, Jianwei Chen, Lynn Hsiao Su, Krystle J. Nomie, Feng Li, Meng C. Wang, Xiaokun Shu, José N. Onuchic, Jennifer A. Woyach, Michael L. Wang, Jin Wang |
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Formato: | article |
Lenguaje: | EN |
Publicado: |
Nature Portfolio
2020
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Materias: | |
Acceso en línea: | https://doaj.org/article/4979b2c9fe654e15a019e2b5da2998c8 |
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