Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials

Y Cheng, C He, M Wang, X Ma, F Mo, S Yang… - Signal transduction and …, 2019 - nature.com
Epigenetic alternations concern heritable yet reversible changes in histone or DNA
modifications that regulate gene activity beyond the underlying sequence. Epigenetic …

Epigenetic and post-translational modifications in autophagy: biological functions and therapeutic targets

F Shu, H Xiao, QN Li, XS Ren, ZG Liu, BW Hu… - … and Targeted Therapy, 2023 - nature.com
Autophagy is a conserved lysosomal degradation pathway where cellular components are
dynamically degraded and re-processed to maintain physical homeostasis. However, the …

Targeted in situ genome-wide profiling with high efficiency for low cell numbers

PJ Skene, JG Henikoff, S Henikoff - Nature protocols, 2018 - nature.com
Cleavage under targets and release using nuclease (CUT&RUN) is an epigenomic profiling
strategy in which antibody-targeted controlled cleavage by micrococcal nuclease releases …

FTO plays an oncogenic role in acute myeloid leukemia as a N6-methyladenosine RNA demethylase

Z Li, H Weng, R Su, X Weng, Z Zuo, C Li, H Huang… - Cancer cell, 2017 - cell.com
Summary N 6-Methyladenosine (m 6 A) represents the most prevalent internal modification
in mammalian mRNAs. Despite its functional importance in various fundamental …

The leukaemia stem cell: similarities, differences and clinical prospects in CML and AML

D Vetrie, GV Helgason, M Copland - Nature Reviews Cancer, 2020 - nature.com
For two decades, leukaemia stem cells (LSCs) in chronic myeloid leukaemia (CML) and
acute myeloid leukaemia (AML) have been advanced paradigms for the cancer stem cell …

Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease

KP Bhat, H Ümit Kaniskan, J Jin… - Nature Reviews Drug …, 2021 - nature.com
Protein lysine methylation is a crucial post-translational modification that regulates the
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …

A CRISPR dropout screen identifies genetic vulnerabilities and therapeutic targets in acute myeloid leukemia

K Tzelepis, H Koike-Yusa, E De Braekeleer, Y Li… - Cell reports, 2016 - cell.com
Acute myeloid leukemia (AML) is an aggressive cancer with a poor prognosis, for which
mainstream treatments have not changed for decades. To identify additional therapeutic …

The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia

EM Stein, G Garcia-Manero, DA Rizzieri… - Blood, The Journal …, 2018 - ashpublications.org
Abstract Pinometostat (EPZ-5676) is a first-in-class small-molecule inhibitor of the histone
methyltransferase disrupter of telomeric silencing 1-like (DOT1L). In this phase 1 study …

H2B Lys34 ubiquitination induces nucleosome distortion to stimulate Dot1L activity

H Ai, M Sun, A Liu, Z Sun, T Liu, L Cao, L Liang… - Nature Chemical …, 2022 - nature.com
Ubiquitination-dependent histone crosstalk plays critical roles in chromatin-associated
processes and is highly associated with human diseases. Mechanism studies of the …

Targeting transcription cycles in cancer

SJ Vervoort, JR Devlin, N Kwiatkowski, M Teng… - Nature Reviews …, 2022 - nature.com
Accurate control of gene expression is essential for normal development and dysregulation
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …