Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity

Cullin-RING E3 ligases (CRLs) regulate the turnover of approximately 20% of mammalian cellular proteins. Neddylation of individual cullin proteins is essential for the activation of each CRL. We report herein the discovery of DI-1548 and DI-1859 as two potent, selective and covalent DCN1 inhibitors....

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Detalhes bibliográficos
Publicado no:Nat Commun
Main Authors: Zhou, Haibin, Lu, Jianfeng, Chinnaswamy, Krishnapriya, Stuckey, Jeanne A., Liu, Liu, McEachern, Donna, Yang, Chao-Yie, Bernard, Denzil, Shen, Hong, Rui, Liangyou, Sun, Yi, Wang, Shaomeng
Formato: Artigo
Idioma:Inglês
Publicado em: Nature Publishing Group UK 2021
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8113459/
https://ncbi.nlm.nih.gov/pubmed/33976147
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41467-021-22924-4
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