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

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

Activation of cullin-RING ligases can be inhibited by targeting DCN1, but selective DCN1 inhibitors with in vivo activity are lacking. Here, the authors develop covalent DCN1 inhibitors that selectively and potently inhibit cullin-3 activation and downstream functions in cells and in mice.

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Auteurs principaux: Haibin Zhou, Jianfeng Lu, Krishnapriya Chinnaswamy, Jeanne A. Stuckey, Liu Liu, Donna McEachern, Chao-Yie Yang, Denzil Bernard, Hong Shen, Liangyou Rui, Yi Sun, Shaomeng Wang
Format: article
Langue:EN
Publié: Nature Portfolio 2021
Sujets:
Science
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Accès en ligne:https://doaj.org/article/f1b1354b41f3482fb5e78275ffe16f27
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Résumé:Activation of cullin-RING ligases can be inhibited by targeting DCN1, but selective DCN1 inhibitors with in vivo activity are lacking. Here, the authors develop covalent DCN1 inhibitors that selectively and potently inhibit cullin-3 activation and downstream functions in cells and in mice.

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