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 …

The COMPASS family of histone H3K4 methylases: mechanisms of regulation in development and disease pathogenesis

A Shilatifard - Annual review of biochemistry, 2012 - annualreviews.org
The Saccharomyces cerevisiae Set1/COMPASS was the first histone H3 lysine 4 (H3K4)
methylase identified over 10 years ago. Since then, it has been demonstrated that …

What a difference a hydroxyl makes: mutant IDH,(R)-2-hydroxyglutarate, and cancer

JA Losman, WG Kaelin - Genes & development, 2013 - genesdev.cshlp.org
Mutations in metabolic enzymes, including isocitrate dehydrogenase 1 (IDH1) and IDH2, in
cancer strongly implicate altered metabolism in tumorigenesis. IDH1 and IDH2 catalyze the …

Contrasting roles of histone 3 lysine 27 demethylases in acute lymphoblastic leukaemia

P Ntziachristos, A Tsirigos, GG Welstead, T Trimarchi… - Nature, 2014 - nature.com
T-cell acute lymphoblastic leukaemia (T-ALL) is a haematological malignancy with a dismal
overall prognosis, including a relapse rate of up to 25%, mainly because of the lack of non …

Deletion of KDM6A, a histone demethylase interacting with MLL2, in three patients with Kabuki syndrome

D Lederer, B Grisart, MC Digilio, V Benoit… - The American Journal of …, 2012 - cell.com
Kabuki syndrome (KS) is a rare genetic disease that causes developmental delay and
congenital anomalies. Since the identification of MLL2 mutations as the primary cause of KS …

EZH2 and KDM6A Act as an Epigenetic Switch to Regulate Mesenchymal Stem Cell Lineage Specification

S Hemming, D Cakouros, S Isenmann, L Cooper… - Stem …, 2014 - academic.oup.com
Abstract The methyltransferase, Enhancer of Zeste homology 2 (EZH2), trimethylates histone
3 lysine 27 (H3K27me3) on chromatin and this repressive mark is removed by lysine …

Histone demethylases in development and disease

MT Pedersen, K Helin - Trends in cell biology, 2010 - cell.com
Histone modifications serve as regulatory marks that are instrumental for the control of
transcription and chromatin architecture. Strict regulation of gene expression patterns is …

UTX and UTY demonstrate histone demethylase-independent function in mouse embryonic development

KB Shpargel, T Sengoku, S Yokoyama, T Magnuson - 2012 - journals.plos.org
UTX (KDM6A) and UTY are homologous X and Y chromosome members of the Histone H3
Lysine 27 (H3K27) demethylase gene family. UTX can demethylate H3K27; however, in vitro …

Histone lysine methylation and demethylation pathways in cancer

RA Varier, HTM Timmers - Biochimica et Biophysica Acta (BBA)-Reviews …, 2011 - Elsevier
The genetic changes leading to the development of human cancer are accompanied by
alterations in the structure and modification status of chromatin, which represent powerful …

UTX mutations in human cancer

L Wang, A Shilatifard - Cancer cell, 2019 - cell.com
Ubiquitously transcribed tetratricopeptide repeat on chromosome X (UTX, encoded by
KDM6A) is a histone demethylase that targets di-and tri-methylated histone H3 lysine 27 …