Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy

L Morera, M Lübbert, M Jung - Clinical epigenetics, 2016 - Springer
The term epigenetics is defined as heritable changes in gene expression that are not due to
alterations of the DNA sequence. In the last years, it has become more and more evident …

Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …

The histone demethylase KDM1A sustains the oncogenic potential of MLL-AF9 leukemia stem cells

WJ Harris, X Huang, JT Lynch, GJ Spencer, JR Hitchin… - Cancer cell, 2012 - cell.com
Using a mouse model of human MLL-AF9 leukemia, we identified the lysine-specific
demethylase KDM1A (LSD1 or AOF2) as an essential regulator of leukemia stem cell (LSC) …

Inhibition of histone lysine-specific demethylase 1 elicits breast tumor immunity and enhances antitumor efficacy of immune checkpoint blockade

Y Qin, SN Vasilatos, L Chen, H Wu, Z Cao, Y Fu… - Oncogene, 2019 - nature.com
Immunotherapy strategies have been emerging as powerful weapons against cancer. Early
clinical trials reveal that overall response to immunotherapy is low in breast cancer patients …

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 …

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 …

A systematic review of histone lysine‐specific demethylase 1 and its inhibitors

YC Zheng, J Ma, Z Wang, J Li, B Jiang… - Medicinal research …, 2015 - Wiley Online Library
Histone lysine‐specific demethylase 1 (LSD1) is the first discovered and reported histone
demethylase by Dr. Shi Yang's group in 2004. It is classified as a member of amine oxidase …

LincRNAFEZF1-AS1 represses p21 expression to promote gastric cancer proliferation through LSD1-Mediated H3K4me2 demethylation

Y Liu, R Xia, K Lu, M Xie, F Yang, M Sun, W De… - Molecular cancer, 2017 - Springer
Background Although the prognosis of gastric cancer patients have a favorable progression,
there are some patients with unusual patterns of locoregional and systemic recurrence …

Pharmacological inhibition of LSD1 for cancer treatment

GJ Yang, PM Lei, SY Wong, DL Ma, CH Leung - Molecules, 2018 - mdpi.com
Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can
remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed …

Estrogen receptor signaling as a target for novel breast cancer therapeutics

JM Renoir, V Marsaud, G Lazennec - Biochemical pharmacology, 2013 - Elsevier
In breast cancer (BC) epithelial cells, the mitogenic action of estradiol is transduced through
binding to two receptors, ERα and ERβ, which act as transcription factors. Anti-estrogens …