A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation

Haibin Zhou; Jianfeng Lu; Liu Liu; Denzil Bernard; Chao-Yie Yang; Ester Fernandez-Salas; Krishnapriya Chinnaswamy; Stephanie Layton; Jeanne Stuckey; Qing Yu; Weihua Zhou; Zhenqiang Pan; Yi Sun; Shaomeng Wang

doi:10.1038/s41467-017-01243-7

Nature Communications (Oct 2017)

A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation

Haibin Zhou,
Jianfeng Lu,
Liu Liu,
Denzil Bernard,
Chao-Yie Yang,
Ester Fernandez-Salas,
Krishnapriya Chinnaswamy,
Stephanie Layton,
Jeanne Stuckey,
Qing Yu,
Weihua Zhou,
Zhenqiang Pan,
Yi Sun,
Shaomeng Wang

Affiliations

Haibin Zhou: Department of Internal Medicine, University of Michigan
Jianfeng Lu: Department of Internal Medicine, University of Michigan
Liu Liu: Department of Internal Medicine, University of Michigan
Denzil Bernard: Department of Internal Medicine, University of Michigan
Chao-Yie Yang: Department of Internal Medicine, University of Michigan
Ester Fernandez-Salas: Department of Pathology, University of Michigan
Krishnapriya Chinnaswamy: Life Sciences Institute, University of Michigan
Stephanie Layton: Life Sciences Institute, University of Michigan
Jeanne Stuckey: Life Sciences Institute, University of Michigan
Qing Yu: Institute of Translational Medicine, Zhejiang University School of Medicine
Weihua Zhou: Division of Radiation and Cancer Biology, Department of Radiation Oncology, University of Michigan
Zhenqiang Pan: Department of Oncological Sciences, Mount Sinai School of Medicine
Yi Sun: Division of Radiation and Cancer Biology, Department of Radiation Oncology, University of Michigan
Shaomeng Wang: Department of Internal Medicine, University of Michigan

DOI: https://doi.org/10.1038/s41467-017-01243-7
Journal volume & issue: Vol. 8, no. 1
pp. 1 – 12

Abstract

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Cullins are central components of the ubiquitin-proteosome system and are activated via a neddylation process mediated by the DCN1–UBC12 complex. Here, the authors develop a small molecule inhibitor of the DCN1–UBC12 interaction that specifically blocks cullin 3 neddylation and can be used to probe the cellular function of cullin 3.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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