EZH2-targeted therapies in cancer: hype or a reality

ML Eich, M Athar, JE Ferguson III, S Varambally - Cancer research, 2020 - AACR
Next-generation genomic sequencing has identified multiple novel molecular alterations in
cancer. Since the identification of DNA methylation and histone modification, it has become …

Cancer as a dysregulated epigenome allowing cellular growth advantage at the expense of the host

W Timp, AP Feinberg - Nature Reviews Cancer, 2013 - nature.com
Although at the genetic level cancer is caused by diverse mutations, epigenetic
modifications are characteristic of all cancers, from apparently normal precursor tissue to …

Functional genomic landscape of acute myeloid leukaemia

JW Tyner, CE Tognon, D Bottomly, B Wilmot, SE Kurtz… - Nature, 2018 - nature.com
The implementation of targeted therapies for acute myeloid leukaemia (AML) has been
challenging because of the complex mutational patterns within and across patients as well …

H3K27me3-rich genomic regions can function as silencers to repress gene expression via chromatin interactions

Y Cai, Y Zhang, YP Loh, JQ Tng, MC Lim, Z Cao… - Nature …, 2021 - nature.com
The mechanisms underlying gene repression and silencers are poorly understood. Here we
investigate the hypothesis that H3K27me3-rich regions of the genome, defined from clusters …

Cancer mediates effector T cell dysfunction by targeting microRNAs and EZH2 via glycolysis restriction

E Zhao, T Maj, I Kryczek, W Li, K Wu, L Zhao, S Wei… - Nature …, 2016 - nature.com
Aerobic glycolysis regulates T cell function. However, whether and how primary cancer
alters T cell glycolytic metabolism and affects tumor immunity in cancer patients remains a …

Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

T Ernst, AJ Chase, J Score, CE Hidalgo-Curtis… - Nature …, 2010 - nature.com
Abnormalities of chromosome 7q are common in myeloid malignancies, but no specific
target genes have yet been identified. Here, we describe the finding of homozygous EZH2 …

Covalent histone modifications—miswritten, misinterpreted and mis-erased in human cancers

P Chi, CD Allis, GG Wang - Nature reviews cancer, 2010 - nature.com
Post-translational modification of histones provides an important regulatory platform for
processes such as gene transcription and DNA damage repair. It has become increasingly …

HDAC inhibitors in acute myeloid leukemia

E San José-Enériz, N Gimenez-Camino, X Agirre… - Cancers, 2019 - mdpi.com
Acute myeloid leukemia (AML) is a hematological malignancy characterized by uncontrolled
proliferation, differentiation arrest, and accumulation of immature myeloid progenitors …

Epigenetic modifications as therapeutic targets

TK Kelly, DD De Carvalho, PA Jones - Nature biotechnology, 2010 - nature.com
Epigenetic modifications work in concert with genetic mechanisms to regulate transcriptional
activity in normal tissues and are often dysregulated in disease. Although they are …

Directed targeting of chromatin to the nuclear lamina is mediated by chromatin state and A-type lamins

JC Harr, TR Luperchio, X Wong, E Cohen… - Journal of Cell …, 2015 - rupress.org
Nuclear organization has been implicated in regulating gene activity. Recently, large
developmentally regulated regions of the genome dynamically associated with the nuclear …