Recent Advances with KDM4 Inhibitors and Potential Applications

The histone lysine demethylase 4 (KDM4) family plays an important role in regulating gene transcription, DNA repair, and metabolism. The dysregulation of KDM4 functions is associated with many human disorders, including cancer, obesity, and cardiovascular diseases. Selective and potent KDM4 inhibito...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 65; no. 14; pp. 9564 - 9579
Main Authors Wu, Qiong, Young, Brandon, Wang, Yan, Davidoff, Andrew M., Rankovic, Zoran, Yang, Jun
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 28.07.2022
Subjects
Enzyme Inhibitors - pharmacology
Histone Demethylases - metabolism
Humans
Jumonji Domain-Containing Histone Demethylases - genetics
Jumonji Domain-Containing Histone Demethylases - metabolism
Neoplasms - drug therapy
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Summary:The histone lysine demethylase 4 (KDM4) family plays an important role in regulating gene transcription, DNA repair, and metabolism. The dysregulation of KDM4 functions is associated with many human disorders, including cancer, obesity, and cardiovascular diseases. Selective and potent KDM4 inhibitors may help not only to understand the role of KDM4 in these disorders but also to provide potential therapeutic opportunities. Here, we provide an overview of the field and discuss current status, challenges, and opportunities lying ahead in the development of KDM4-based anticancer therapeutics.
Bibliography:Q.W. and J.Y. wrote the manuscript with help from B.Y., Y.W., Z.R. and A.M.D.
Author contributions.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.2c00680