Targeting transcription factors in cancer—from undruggable to reality

JH Bushweller - Nature Reviews Cancer, 2019 - nature.com
Mutated or dysregulated transcription factors represent a unique class of drug targets that
mediate aberrant gene expression, including blockade of differentiation and cell death gene …

Lineage-specific and single-cell chromatin accessibility charts human hematopoiesis and leukemia evolution

MR Corces, JD Buenrostro, B Wu, PG Greenside… - Nature …, 2016 - nature.com
We define the chromatin accessibility and transcriptional landscapes in 13 human primary
blood cell types that span the hematopoietic hierarchy. Exploiting the finding that the …

Subtype-specific regulatory network rewiring in acute myeloid leukemia

SA Assi, MR Imperato, DJL Coleman, A Pickin… - Nature …, 2019 - nature.com
Acute myeloid leukemia (AML) is a heterogeneous disease caused by a variety of
alterations in transcription factors, epigenetic regulators and signaling molecules. To …

[HTML][HTML] Molecular basis of hematological disease caused by inherited or acquired RUNX1 mutations

SG Kellaway, DJL Coleman, PN Cockerill… - Experimental …, 2022 - Elsevier
Highlights•Germline and acquired RUNX1 mutations are associated with FPD and
MDS/AML.•Large deletions and nonsense mutations are more common in germline FPD …

RIPK3 restricts myeloid leukemogenesis by promoting cell death and differentiation of leukemia initiating cells

U Höckendorf, M Yabal, T Herold, E Munkhbaatar… - Cancer cell, 2016 - cell.com
Since acute myeloid leukemia (AML) is characterized by the blockade of hematopoietic
differentiation and cell death, we interrogated RIPK3 signaling in AML development. Genetic …

Inhibition of the succinyl dehydrogenase complex in acute myeloid leukemia leads to a lactate-fuelled respiratory metabolic vulnerability

A Erdem, S Marin, DA Pereira-Martins… - Nature …, 2022 - nature.com
Metabolic programs can differ substantially across genetically distinct subtypes of acute
myeloid leukemia (AML). These programs are not static entities but can change swiftly as a …

Prospective isolation and characterization of genetically and functionally distinct AML subclones

B de Boer, J Prick, MG Pruis, P Keane, MR Imperato… - Cancer cell, 2018 - cell.com
Intra-tumor heterogeneity caused by clonal evolution is a major problem in cancer treatment.
To address this problem, we performed label-free quantitative proteomics on primary acute …

Transcriptional reprogramming by mutated IRF4 in lymphoma

N Schleussner, P Cauchy, V Franke, M Giefing… - Nature …, 2023 - nature.com
Disease-causing mutations in genes encoding transcription factors (TFs) can affect TF
interactions with their cognate DNA-binding motifs. Whether and how TF mutations impact …

[HTML][HTML] Gene regulatory network analysis predicts cooperating transcription factor regulons required for FLT3-ITD+ AML growth

DJL Coleman, P Keane, R Luque-Martin, PS Chin… - Cell reports, 2023 - cell.com
Acute myeloid leukemia (AML) is a heterogeneous disease caused by different mutations.
Previously, we showed that each mutational subtype develops its specific gene regulatory …

Mutational synergy during leukemia induction remodels chromatin accessibility, histone modifications and three-dimensional DNA topology to alter gene expression

H Yun, N Narayan, S Vohra, G Giotopoulos, A Mupo… - Nature …, 2021 - nature.com
Altered transcription is a cardinal feature of acute myeloid leukemia (AML); however, exactly
how mutations synergize to remodel the epigenetic landscape and rewire three-dimensional …