The impact of cellular metabolism on chromatin dynamics and epigenetics

MA Reid, Z Dai, JW Locasale - Nature cell biology, 2017 - nature.com
The substrates used to modify nucleic acids and chromatin are affected by nutrient
availability and the activity of metabolic pathways. Thus, cellular metabolism constitutes a …

Targeting metalloenzymes for therapeutic intervention

AY Chen, RN Adamek, BL Dick, CV Credille… - Chemical …, 2018 - ACS Publications
Metalloenzymes are central to a wide range of essential biological activities, including
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …

Epigenetic protein families: a new frontier for drug discovery

CH Arrowsmith, C Bountra, PV Fish, K Lee… - Nature reviews Drug …, 2012 - nature.com
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …

The oncometabolite 2‐hydroxyglutarate inhibits histone lysine demethylases

R Chowdhury, KK Yeoh, YM Tian, L Hillringhaus… - EMBO …, 2011 - embopress.org
Mutations in isocitrate dehydrogenases (IDHs) have a gain‐of‐function effect leading to R
(−)‐2‐hydroxyglutarate (R‐2HG) accumulation. By using biochemical, structural and cellular …

Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J Jin - Chemical reviews, 2018 - ACS Publications
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

[HTML][HTML] Metabolic regulation of epigenetics

C Lu, CB Thompson - Cell metabolism, 2012 - cell.com
How cells sense and respond to environmental cues remains a central question of biological
research. Recent evidence suggests that DNA transcription is regulated by chromatin …

Histone lysine demethylases as targets for anticancer therapy

JW Højfeldt, K Agger, K Helin - Nature reviews Drug discovery, 2013 - nature.com
It has recently been demonstrated that the genes controlling the epigenetic programmes that
are required for maintaining chromatin structure and cell identity include genes that drive …

Epigenetics in cancer: fundamentals and beyond

S Biswas, CM Rao - Pharmacology & Therapeutics, 2017 - Elsevier
Activation of oncogenes or the deactivation of tumor suppressor genes has long been
established as the fundamental mechanism leading towards carcinogenesis. Although this …

The emerging role of KDM5A in human cancer

GJ Yang, MH Zhu, XJ Lu, YJ Liu, JF Lu… - Journal of hematology & …, 2021 - Springer
Histone methylation is a key posttranslational modification of chromatin, and its
dysregulation affects a wide array of nuclear activities including the maintenance of genome …

Arginine demethylation is catalysed by a subset of JmjC histone lysine demethylases

LJ Walport, RJ Hopkinson, R Chowdhury… - Nature …, 2016 - nature.com
While the oxygen-dependent reversal of lysine N ɛ-methylation is well established, the
existence of bona fide N ω-methylarginine demethylases (RDMs) is controversial. Lysine …