Targeting transcription factors for cancer treatment

M Lambert, S Jambon, S Depauw… - Molecules, 2018 - mdpi.com
Transcription factors are involved in a large number of human diseases such as cancers for
which they account for about 20% of all oncogenes identified so far. For long time, with the …

MLL-rearranged leukemias—an update on science and clinical approaches

AC Winters, KM Bernt - Frontiers in pediatrics, 2017 - frontiersin.org
The mixed-lineage leukemia 1 (MLL1) gene (now renamed Lysine [K]-specific
MethylTransferase 2A or KMT2A) on chromosome 11q23 is disrupted in a unique group of …

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 …

Inhibition of histone deacetylases in cancer therapy: lessons from leukaemia

E Ceccacci, S Minucci - British journal of cancer, 2016 - nature.com
Histone deacetylases (HDACs) are a key component of the epigenetic machinery regulating
gene expression, and behave as oncogenes in several cancer types, spurring the …

Targeting histone acetylation dynamics and oncogenic transcription by catalytic P300/CBP inhibition

SJ Hogg, O Motorna, LA Cluse, TM Johanson… - Molecular cell, 2021 - cell.com
To separate causal effects of histone acetylation on chromatin accessibility and
transcriptional output, we used integrated epigenomic and transcriptomic analyses following …

[HTML][HTML] Functional genomics identify distinct and overlapping genes mediating resistance to different classes of heterobifunctional degraders of oncoproteins

R Shirasaki, GM Matthews, S Gandolfi… - Cell Reports, 2021 - cell.com
Heterobifunctional proteolysis-targeting chimeric compounds leverage the activity of E3
ligases to induce degradation of target oncoproteins and exhibit potent preclinical antitumor …

HDAC3 inhibition upregulates PD-L1 expression in B-cell lymphomas and augments the efficacy of anti–PD-L1 therapy

S Deng, Q Hu, H Zhang, F Yang, C Peng… - Molecular cancer …, 2019 - AACR
Programmed cell-death protein 1 (PD-1) and programmed death-ligand 1 (PD-L1) pathway
blockade is a promising therapy for the treatment of advanced cancers, including B-cell …

Surface antigen-guided CRISPR screens identify regulators of myeloid leukemia differentiation

E Wang, H Zhou, B Nadorp, G Cayanan, X Chen… - Cell Stem Cell, 2021 - cell.com
Lack of cellular differentiation is a hallmark of many human cancers, including acute myeloid
leukemia (AML). Strategies to overcome such a differentiation blockade are an approach for …

Potent hydrazide-based HDAC inhibitors with a superior pharmacokinetic profile for efficient treatment of acute myeloid leukemia in vivo

Y Jiang, J Xu, K Yue, C Huang, M Qin… - Journal of Medicinal …, 2021 - ACS Publications
As “Michael acceptors” may induce promiscuous responses in mammalian cells by reacting
with various proteins, we modified the cinnamamide of our previous hydrazide-based HDAC …

A chemical probe toolbox for dissecting the cancer epigenome

J Shortt, CJ Ott, RW Johnstone, JE Bradner - Nature Reviews Cancer, 2017 - nature.com
Cancer cell hallmarks are underpinned by transcriptional programmes operating in the
context of a dynamic and complicit epigenomic environment. Somatic alterations of …