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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Autores principales: 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
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Lenguaje:EN
Publicado: Nature Portfolio 2021
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Acceso en línea:https://doaj.org/article/f1b1354b41f3482fb5e78275ffe16f27
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spelling oai:doaj.org-article:f1b1354b41f3482fb5e78275ffe16f272021-12-02T15:36:28ZSelective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity10.1038/s41467-021-22924-42041-1723https://doaj.org/article/f1b1354b41f3482fb5e78275ffe16f272021-05-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-22924-4https://doaj.org/toc/2041-1723Activation 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.Haibin ZhouJianfeng LuKrishnapriya ChinnaswamyJeanne A. StuckeyLiu LiuDonna McEachernChao-Yie YangDenzil BernardHong ShenLiangyou RuiYi SunShaomeng WangNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-13 (2021)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
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
Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity
description 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.
format article
author 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
author_facet 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
author_sort Haibin Zhou
title Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity
title_short Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity
title_full Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity
title_fullStr Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity
title_full_unstemmed Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity
title_sort selective inhibition of cullin 3 neddylation through covalent targeting dcn1 protects mice from acetaminophen-induced liver toxicity
publisher Nature Portfolio
publishDate 2021
url https://doaj.org/article/f1b1354b41f3482fb5e78275ffe16f27
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