Small molecule KDM4s inhibitors as anti-cancer agents

H Lin, Q Li, Q Li, J Zhu, K Gu, X Jiang… - Journal of Enzyme …, 2018 - Taylor & Francis
Histone demethylation is a vital process in epigenetic regulation of gene expression. A
number of histone demethylases are present to control the methylated states of histone …

KDM4 histone demethylase inhibitors for anti-cancer agents: a patent review

YW Chin, SY Han - Expert opinion on therapeutic patents, 2015 - Taylor & Francis
Introduction: As epigenetic modulators, histone demethylases can be a therapeutic target in
the area of oncology. KDM4 subfamily proteins are histone demethylases with a Jumonji …

Unravelling KDM4 histone demethylase inhibitors for cancer therapy

S Baby, DG Valapil, N Shankaraiah - Drug discovery today, 2021 - Elsevier
Epigenetic enzyme-targeted therapy is a promising new development in the field of drug
discovery. To date, histone deacetylases and DNA methyltransferases have been …

Recent advances with KDM4 inhibitors and potential applications

Q Wu, B Young, Y Wang, AM Davidoff… - Journal of medicinal …, 2022 - ACS Publications
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 …

Advances in histone demethylase KDM3A as a cancer therapeutic target

J Yoo, YH Jeon, HY Cho, SW Lee, GW Kim, DH Lee… - Cancers, 2020 - mdpi.com
Lysine-specific histone demethylase 3 (KDM3) subfamily proteins are H3K9me2/me1
histone demethylases that promote gene expression. The KDM3 subfamily primarily consists …

Advances in histone demethylase KDM4 as cancer therapeutic targets

DH Lee, GW Kim, YH Jeon, J Yoo, SW Lee… - The FASEB …, 2020 - Wiley Online Library
Abstract The KDM4 subfamily H3K9 histone demethylases are epigenetic regulators that
control chromatin structure and gene expression by demethylating histone H3K9, H3K36 …

Development of JmjC-domain-containing histone demethylase (KDM2-7) inhibitors for cancer therapy

L Zhang, Y Chen, Z Li, C Lin, T Zhang, G Wang - Drug Discovery Today, 2023 - Elsevier
Highlights•The dysregulation of JmjC-KDMs is closely related with various human diseases,
especially cancers.•The structures and transcriptional regulation of JmjC-KDMs are …

Discovery of a potent and selective inhibitor of histone lysine demethylase KDM4D

Z Fang, Y Liu, R Zhang, Q Chen, T Wang… - European Journal of …, 2021 - Elsevier
Histone lysine demethylase 4D (KDM4D) plays an important role in the regulation of
tumorigenesis, progression and drug resistance and has been considered a potential target …

Lysine demethylase 5B (KDM5B): A potential anti-cancer drug target

YC Zheng, J Chang, LC Wang, HM Ren… - European Journal of …, 2019 - Elsevier
Abstract Lysine demethylase 5B (KDM5B) is a histone demethylase identified in 2007, which
is responsible for erasing H3K4me2/3 activation marker. It participates in multiple repressive …

Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present)

X He, H Zhang, Y Zhang, Y Ye, S Wang, R Bai… - European Journal of …, 2022 - Elsevier
Post-translational modifications (PTMs) of histone by histone demethylases (KDMs) play an
important role in the regulation of gene expression, which implicates the development of …