Recent Advances with KDM4 Inhibitors and Potential Applications

J Med Chem. 2022 Jul 15. doi: 10.1021/acs.jmedchem.2c00680. Online ahead of print.


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.

PMID:35838529 | DOI:10.1021/acs.jmedchem.2c00680

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