An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells

M Vinogradova, VS Gehling, A Gustafson… - Nature chemical …, 2016 - nature.com
The KDM5 family of histone demethylases catalyzes the demethylation of histone H3 on
lysine 4 (H3K4) and is required for the survival of drug-tolerant persister cancer cells (DTPs) …

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 …

[HTML][HTML] Histone lysine demethylase (KDM) subfamily 4: structures, functions and therapeutic potential

RM Labbé, A Holowatyj, ZQ Yang - American journal of …, 2014 - ncbi.nlm.nih.gov
KDM4 histone demethylases catalyze the removal of methyl marks from histone lysine
residues to epigenetically regulate chromatin structure and gene expression. KDM4 …

KDM5 demethylases and their role in cancer cell chemoresistance

J Plch, J Hrabeta, T Eckschlager - International journal of …, 2019 - Wiley Online Library
Histone methylation is important in the regulation of genes expression, and thus its
dysregulation has been observed in various cancers. KDM5 enzymes are capable of …

Structural analysis of human KDM5B guides histone demethylase inhibitor development

C Johansson, S Velupillai, A Tumber… - Nature chemical …, 2016 - nature.com
Members of the KDM5 (also known as JARID1) family are 2-oxoglutarate-and Fe2+-
dependent oxygenases that act as histone H3K4 demethylases, thereby regulating cell …

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity

T Suzuki, H Ozasa, Y Itoh, P Zhan… - Journal of medicinal …, 2013 - ACS Publications
Histone N ε-methyl lysine demethylases KDM2/7 have been identified as potential targets for
cancer therapies. On the basis of the crystal structure of KDM7B, we designed and prepared …

[HTML][HTML] The critical role of histone lysine demethylase KDM2B in cancer

M Yan, X Yang, H Wang, Q Shao - American journal of …, 2018 - ncbi.nlm.nih.gov
The discovery of histone demethylases has revealed the dynamic nature of the regulation of
histone methylation. KDM2B is an important histone lysine demethylase that removes methyl …

The role of the histone demethylase KDM4A in cancer

L Guerra-Calderas, R González-Barrios, LA Herrera… - Cancer genetics, 2015 - Elsevier
Histone posttranslational modifications are important components of epigenetic regulation.
One extensively studied modification is the methylation of lysine residues. These …

[HTML][HTML] Genomic amplification and a role in drug-resistance for the KDM5A histone demethylase in breast cancer

J Hou, J Wu, A Dombkowski, K Zhang… - American journal of …, 2012 - ncbi.nlm.nih.gov
Lysine-specific demethylase 5A (KDM5A), an enzyme that removes activating H3K4 di-and
trimethylation marks, plays critical roles in controlling transcription and chromatin …