Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials

Y Cheng, C He, M Wang, X Ma, F Mo, S Yang… - Signal transduction and …, 2019 - nature.com
Epigenetic alternations concern heritable yet reversible changes in histone or DNA
modifications that regulate gene activity beyond the underlying sequence. Epigenetic …

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 …

2-Oxoglutarate-dependent oxygenases

MS Islam, TM Leissing, R Chowdhury… - Annual review of …, 2018 - annualreviews.org
2-Oxoglutarate (2OG)-dependent oxygenases (2OGXs) catalyze a remarkably diverse range
of oxidative reactions. In animals, these comprise hydroxylations and N-demethylations …

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 …

Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials

TL Yeh, TM Leissing, MI Abboud, CC Thinnes… - Chemical …, 2017 - pubs.rsc.org
Inhibition of the human 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl
hydroxylases (human PHD1–3) causes upregulation of HIF, thus promoting erythropoiesis …

Functional role of G9a histone methyltransferase in cancer

F Casciello, K Windloch, F Gannon, JS Lee - Frontiers in immunology, 2015 - frontiersin.org
Post-translational modifications of DNA and histones are epigenetic mechanisms, which
affect the chromatin structure, ultimately leading to gene expression changes. A number of …

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 …

Human UTY (KDM6C) is a male-specific Nϵ-methyl lysyl demethylase

LJ Walport, RJ Hopkinson, M Vollmar… - Journal of Biological …, 2014 - ASBMB
The Jumonji C lysine demethylases (KDMs) are 2-oxoglutarate-and Fe (II)-dependent
oxygenases. KDM6A (UTX) and KDM6B (JMJD3) are KDM6 subfamily members that …

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 …

Targeting histone lysine methylation in cancer

J McGrath, P Trojer - Pharmacology & therapeutics, 2015 - Elsevier
Within the vast landscape of histone modifications lysine methylation has gained increasing
attention because of its profound regulatory potential. The methylation of lysine residues on …