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Advances in Histone Demethylase KDM3A as a Cancer Therapeutic Target

1
College of Pharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 21983, Korea
2
Department of Integrated OMICS for Biomedical Science, Yonsei University, Seoul 03722, Korea
*
Author to whom correspondence should be addressed.
Cancers 2020, 12(5), 1098; https://doi.org/10.3390/cancers12051098
Received: 6 April 2020 / Revised: 24 April 2020 / Accepted: 27 April 2020 / Published: 28 April 2020
(This article belongs to the Special Issue Epigenetic Therapy: The State of Play in Highly Aggressive Diseases)
Lysine-specific histone demethylase 3 (KDM3) subfamily proteins are H3K9me2/me1 histone demethylases that promote gene expression. The KDM3 subfamily primarily consists of four proteins (KDM3A−D). All four proteins contain the catalytic Jumonji C domain (JmjC) at their C-termini, but whether KDM3C has demethylase activity is under debate. In addition, KDM3 proteins contain a zinc-finger domain for DNA binding and an LXXLL motif for interacting with nuclear receptors. Of the KDM3 proteins, KDM3A is especially deregulated or overexpressed in multiple cancers, making it a potential cancer therapeutic target. However, no KDM3A-selective inhibitors have been identified to date because of the lack of structural information. Uncovering the distinct physiological and pathological functions of KDM3A and their structure will give insight into the development of novel selective inhibitors. In this review, we focus on recent studies highlighting the oncogenic functions of KDM3A in cancer. We also discuss existing KDM3A-related inhibitors and review their potential as therapeutic agents for overcoming cancer. View Full-Text
Keywords: KDM3A; histone H3K9 demethylase; KDM3 inhibitor; anti-cancer agent; epigenetic agent KDM3A; histone H3K9 demethylase; KDM3 inhibitor; anti-cancer agent; epigenetic agent
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Yoo, J.; Jeon, Y.H.; Cho, H.Y.; Lee, S.W.; Kim, G.W.; Lee, D.H.; Kwon, S.H. Advances in Histone Demethylase KDM3A as a Cancer Therapeutic Target. Cancers 2020, 12, 1098.

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