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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Nature Portfolio
2021
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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) |
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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 |
work_keys_str_mv |
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