Epigenetics in cancer stem cells

TB Toh, JJ Lim, EKH Chow - Molecular cancer, 2017 - Springer
Compelling evidence have demonstrated that bulk tumors can arise from a unique subset of
cells commonly termed “cancer stem cells” that has been proposed to be a strong driving …

Epigenetics and approaches to targeted epigenetic therapy in acute myeloid leukemia

BJ Wouters, R Delwel - Blood, The Journal of the American …, 2016 - ashpublications.org
Acute myeloid leukemia (AML) is the most common type of acute leukemia in adults. AML is
a heterogeneous malignancy characterized by distinct genetic abnormalities. Recent …

A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC

HP Mohammad, KN Smitheman, CD Kamat, D Soong… - Cancer cell, 2015 - cell.com
Epigenetic dysregulation has emerged as an important mechanism in cancer. Alterations in
epigenetic machinery have become a major focus for targeted therapies. The current report …

Targeting long non-coding RNAs in cancers: progress and prospects

CH Li, Y Chen - The international journal of biochemistry & cell biology, 2013 - Elsevier
Pervasive transcription occurs in the human genome to generate thousands of RNA
transcripts, and accumulating evidence suggested that the RNA molecules, without protein …

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 …

Enhancer activation by pharmacologic displacement of LSD1 from GFI1 induces differentiation in acute myeloid leukemia

A Maiques-Diaz, GJ Spencer, JT Lynch, F Ciceri… - Cell reports, 2018 - cell.com
Pharmacologic inhibition of LSD1 promotes blast cell differentiation in acute myeloid
leukemia (AML) with MLL translocations. The assumption has been that differentiation is …

LSD1: biologic roles and therapeutic targeting

A Maiques-Diaz, TCP Somervaille - Epigenomics, 2016 - Taylor & Francis
LSD1 (KDM1A; BHC110; AOF2) was the first protein reported to exhibit histone demethylase
activity and has since been shown to have multiple essential roles in mammalian biology …

Long non-coding RNA HOTAIR promotes glioblastoma cell cycle progression in an EZH2 dependent manner

K Zhang, X Sun, X Zhou, L Han, L Chen, Z Shi… - …, 2014 - pmc.ncbi.nlm.nih.gov
The long non-coding RNA Hox transcript antisense intergenic RNA (HOTAIR) was recently
implicated in breast cancer metastasis and is predictive of poor prognosis in colorectal and …

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 …

First-in-human phase I study of iadademstat (ORY-1001): a first-in-class lysine-specific histone demethylase 1A inhibitor, in relapsed or refractory acute myeloid …

O Salamero, P Montesinos, C Willekens… - Journal of Clinical …, 2020 - ascopubs.org
PURPOSE Iadademstat is a novel, highly potent, and selective inhibitor of LSD1 (KDM1A),
with preclinical in vitro and in vivo antileukemic activity. This study aimed to determine safety …