Histone lysine demethylases as targets for anticancer therapy

JW Højfeldt, K Agger, K Helin - Nature reviews Drug discovery, 2013 - nature.com
It has recently been demonstrated that the genes controlling the epigenetic programmes that
are required for maintaining chromatin structure and cell identity include genes that drive …

Chromatin proteins and modifications as drug targets

K Helin, D Dhanak - Nature, 2013 - nature.com
A plethora of groundbreaking studies have demonstrated the importance of chromatin-
associated proteins and post-translational modifications of histones, proteins and DNA (so …

An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1

KD Konze, A Ma, F Li, D Barsyte-Lovejoy… - ACS chemical …, 2013 - ACS Publications
EZH2 or EZH1 is the catalytic subunit of the polycomb repressive complex 2 that catalyzes
methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a …

Emerging roles for chromatin as a signal integration and storage platform

AI Badeaux, Y Shi - Nature reviews Molecular cell biology, 2013 - nature.com
Cells of a multicellular organism, all containing nearly identical genetic information, respond
to differentiation cues in variable ways. In addition, cells are plastic, able to execute their …

[HTML][HTML] The histone LSD1 demethylase in stemness and cancer transcription programs

S Amente, L Lania, B Majello - Biochimica et Biophysica Acta (BBA)-Gene …, 2013 - Elsevier
DNA and histone chromatin modifying enzymes play a crucial role in chromatin remodeling
in several biological processes. Lysine-specific demethylase 1 (LSD1), the first identified …

Triazole–dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration

YC Zheng, YC Duan, JL Ma, RM Xu, X Zi… - Journal of medicinal …, 2013 - ACS Publications
Lysine specific demethylase 1 (LSD1), the first identified histone demethylase, plays an
important role in epigenetic regulation of gene activation and repression. The up-regulated …

LSD1-mediated epigenetic modification contributes to proliferation and metastasis of colon cancer

J Ding, ZM Zhang, Y Xia, GQ Liao, Y Pan, S Liu… - British journal of …, 2013 - nature.com
Background: Emerging evidence has demonstrated that lysine-specific demethylase 1
(LSD1) has an important role in many pathological processes of cancer cells, such as …

Regulation of estrogen receptor α by histone methyltransferase SMYD2-mediated protein methylation

X Zhang, K Tanaka, J Yan, J Li… - Proceedings of the …, 2013 - National Acad Sciences
Estrogen receptor alpha (ERα) is a ligand-activated transcription factor. Upon estrogen
stimulation, ERα recruits a number of coregulators, including both coactivators and …

Inhibiting interactions of lysine demethylase LSD1 with snail/slug blocks cancer cell invasion

G Ferrari-Amorotti, V Fragliasso, R Esteki, Z Prudente… - Cancer research, 2013 - AACR
The process of epithelial–mesenchymal transition (EMT) which is required for cancer cell
invasion is regulated by a family of E-box–binding transcription repressors, which include …

[HTML][HTML] The lysine specific demethylase-1 (LSD1/KDM1A) regulates VEGF-A expression in prostate cancer

V Kashyap, S Ahmad, EM Nilsson, L Helczynski… - Molecular …, 2013 - Elsevier
Recurrent prostate cancer remains a major clinical challenge. The lysine specific
demethylase-1 (LSD1/KDM1A), together with the JmjC domain-containing JMJD2A and …