RNA N6-methyladenosine modification in cancers: current status and perspectives

X Deng, R Su, H Weng, H Huang, Z Li, J Chen - Cell research, 2018 - nature.com
Abstract N 6-methyladenosine (m6A), the most abundant internal modification in eukaryotic
messenger RNAs (mRNAs), has been shown to play critical roles in various normal …

Drugging the undruggable RAS: Mission possible?

AD Cox, SW Fesik, AC Kimmelman, J Luo… - Nature reviews Drug …, 2014 - nature.com
Despite more than three decades of intensive effort, no effective pharmacological inhibitors
of the RAS oncoproteins have reached the clinic, prompting the widely held perception that …

Recent progress of targeted G-quadruplex-preferred ligands toward cancer therapy

S Asamitsu, S Obata, Z Yu, T Bando, H Sugiyama - Molecules, 2019 - mdpi.com
A G-quadruplex (G4) is a well-known nucleic acid secondary structure comprising guanine-
rich sequences, and has profound implications for various pharmacological and biological …

Transcriptional plasticity promotes primary and acquired resistance to BET inhibition

P Rathert, M Roth, T Neumann, F Muerdter, JS Roe… - Nature, 2015 - nature.com
Following the discovery of BRD4 as a non-oncogene addiction target in acute myeloid
leukaemia (AML),, bromodomain and extra terminal protein (BET) inhibitors are being …

An optimized microRNA backbone for effective single-copy RNAi

C Fellmann, T Hoffmann, V Sridhar, B Hopfgartner… - Cell reports, 2013 - cell.com
Short hairpin RNA (shRNA) technology enables stable and regulated gene repression. For
establishing experimentally versatile RNAi tools and minimizing toxicities, synthetic shRNAs …

BET bromodomain inhibition as a therapeutic strategy to target c-Myc

JE Delmore, GC Issa, ME Lemieux, PB Rahl, J Shi… - Cell, 2011 - cell.com
MYC contributes to the pathogenesis of a majority of human cancers, yet strategies to
modulate the function of the c-Myc oncoprotein do not exist. Toward this objective, we have …

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

J Zuber, J Shi, E Wang, AR Rappaport, H Herrmann… - Nature, 2011 - nature.com
Epigenetic pathways can regulate gene expression by controlling and interpreting chromatin
modifications. Cancer cells are characterized by altered epigenetic landscapes, and …

Role of SWI/SNF in acute leukemia maintenance and enhancer-mediated Myc regulation

J Shi, WA Whyte, CJ Zepeda-Mendoza… - Genes & …, 2013 - genesdev.cshlp.org
Cancer cells frequently depend on chromatin regulatory activities to maintain a malignant
phenotype. Here, we show that leukemia cells require the mammalian SWI/SNF chromatin …

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) …

Differentiation therapy revisited

H de Thé - Nature Reviews Cancer, 2018 - nature.com
The concept of differentiation therapy emerged from the fact that hormones or cytokines may
promote differentiation ex vivo, thereby irreversibly changing the phenotype of cancer cells …