Targeting the epigenetic regulation of antitumour immunity

SJ Hogg, PA Beavis, MA Dawson… - Nature reviews Drug …, 2020 - nature.com
Dysregulation of the epigenome drives aberrant transcriptional programmes that promote
cancer onset and progression. Although defective gene regulation often affects oncogenic …

Marked for death: targeting epigenetic changes in cancer

SX Pfister, A Ashworth - Nature reviews Drug discovery, 2017 - nature.com
In the past few years, it has become clear that mutations in epigenetic regulatory genes are
common in human cancers. Therapeutic strategies are now being developed to target …

Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells

W Fiskus, S Sharma, B Shah, BP Portier, SGT Devaraj… - Leukemia, 2014 - nature.com
The histone demethylase LSD1 (KDM1A) demethylates mono-and di-methylated (Me2)
lysine (K) 4 on histone H3. High LSD1 expression blocks differentiation and confers a poor …

Transposable element regulation and expression in cancer

EE Grundy, N Diab, KB Chiappinelli - The FEBS journal, 2022 - Wiley Online Library
Approximately 45% of the human genome is composed of transposable elements (TEs).
Expression of these elements is tightly regulated during normal development. TEs may be …

[HTML][HTML] Epigenetics in hepatocellular carcinoma development and therapy: The tip of the iceberg

MG Fernández-Barrena, M Arechederra, L Colyn… - Jhep Reports, 2020 - Elsevier
Hepatocellular carcinoma (HCC) is a deadly tumour whose causative agents are generally
well known, but whose pathogenesis remains poorly understood. Nevertheless, key genetic …

Emerging epigenetic‐based nanotechnology for cancer therapy: modulating the tumor microenvironment

J Zhang, L Huang, G Ge, K Hu - Advanced Science, 2023 - Wiley Online Library
Dysregulated epigenetic modifications dynamically drive the abnormal transcription process
to affect the tumor microenvironment; thus, promoting cancer progression, drug resistance …

High-Throughput Virtual Screening Identifies Novel N′-(1-Phenylethylidene)-benzohydrazides as Potent, Specific, and Reversible LSD1 Inhibitors

V Sorna, ER Theisen, B Stephens… - Journal of medicinal …, 2013 - ACS Publications
Lysine specific demethylase 1 (LSD1) plays an important role in regulating histone lysine
methylation at residues K4 and K9 on histone H3 and is an attractive therapeutic target in …

Therapeutic strategies targeting cancer stem cells and their microenvironment

HR Sun, S Wang, SC Yan, Y Zhang, PJ Nelson… - Frontiers in …, 2019 - frontiersin.org
Cancer stem cells (CSCs) have been demonstrated in a variety of tumors and are thought to
act as a clonogenic core for the genesis of new tumor growth. This small subpopulation of …

Reversible LSD1 inhibition interferes with global EWS/ETS transcriptional activity and impedes Ewing sarcoma tumor growth

S Sankar, ER Theisen, J Bearss, T Mulvihill… - Clinical cancer …, 2014 - AACR
Purpose: Ewing sarcoma is a pediatric bone tumor that absolutely relies on the
transcriptional activity of the EWS/ETS family of fusion oncoproteins. While the most common …

Epigenetics in ovarian cancer: premise, properties, and perspectives

Q Yang, Y Yang, N Zhou, K Tang, WB Lau, B Lau… - Molecular cancer, 2018 - Springer
Malignant ovarian tumors bear the highest mortality rate among all gynecological cancers.
Both late tumor diagnosis and tolerance to available chemical therapy increase patient …