Histone demethylases in chromatin biology and beyond

E Dimitrova, AH Turberfield, RJ Klose - EMBO reports, 2015 - embopress.org
Histone methylation plays fundamental roles in regulating chromatin‐based processes. With
the discovery of histone demethylases over a decade ago, it is now clear that histone …

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 …

Multi-omics analyses of the ulcerative colitis gut microbiome link Bacteroides vulgatus proteases with disease severity

RH Mills, PS Dulai, Y Vázquez-Baeza, C Sauceda… - Nature …, 2022 - nature.com
Ulcerative colitis (UC) is driven by disruptions in host–microbiota homoeostasis, but current
treatments exclusively target host inflammatory pathways. To understand how host …

IDH-mutated gliomas promote epileptogenesis through d-2-hydroxyglutarate-dependent mTOR hyperactivation

A Mortazavi, I Fayed, M Bachani, T Dowdy… - Neuro …, 2022 - academic.oup.com
Background Uncontrolled seizures in patients with gliomas have a significant impact on
quality of life and morbidity, yet the mechanisms through which these tumors cause seizures …

[HTML][HTML] Histone demethylases and their roles in cancer epigenetics

A D'Oto, Q Tian, AM Davidoff, J Yang - Journal of medical oncology …, 2016 - ncbi.nlm.nih.gov
The genetic abnormalities that drive tumorigenesis are usually coupled with epigenetic
alterations, such as DNA methylation and aberrant histone modifications, which may help …

Histone demethylase JMJD2A drives prostate tumorigenesis through transcription factor ETV1

TD Kim, F Jin, S Shin, S Oh… - The Journal of …, 2016 - Am Soc Clin Investig
Histone demethylase upregulation has been observed in human cancers, yet it is unknown
whether this is a bystander event or a driver of tumorigenesis. We found that overexpression …

Lysine methylation regulators moonlighting outside the epigenome

EM Cornett, L Ferry, PA Defossez, SB Rothbart - Molecular cell, 2019 - cell.com
Landmark discoveries made nearly two decades ago identified known transcriptional
regulators as histone lysine methyltransferases. Since then, the field of lysine methylation …

Characterization of a linked Jumonji domain of the KDM5/JARID1 family of histone H3 lysine 4 demethylases

JR Horton, A Engstrom, EL Zoeller, X Liu… - Journal of Biological …, 2016 - ASBMB
The KDM5/JARID1 family of Fe (II)-and α-ketoglutarate-dependent demethylases remove
methyl groups from tri-and dimethylated lysine 4 of histone H3. Accumulating evidence from …

Structure-based optimization of potent, selective, and orally bioavailable CDK8 inhibitors discovered by high-throughput screening

P Czodrowski, A Mallinger, D Wienke… - Journal of medicinal …, 2016 - ACS Publications
The mediator complex-associated cyclin dependent kinase CDK8 regulates β-catenin-
dependent transcription following activation of WNT signaling. Multiple lines of evidence …

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 …