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 …

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 …

FcγR engagement reprograms neutrophils into antigen cross-presenting cells that elicit acquired anti-tumor immunity

V Mysore, X Cullere, J Mears, F Rosetti… - Nature …, 2021 - nature.com
Classical dendritic cells (cDC) are professional antigen-presenting cells (APC) that regulate
immunity and tolerance. Neutrophil-derived cells with properties of DCs (nAPC) are …

PTEN tumor-suppressor: the dam of stemness in cancer

F Luongo, F Colonna, F Calapà, S Vitale, ME Fiori… - Cancers, 2019 - mdpi.com
PTEN is one of the most frequently inactivated tumor suppressor genes in cancer. Loss or
variation in PTEN gene/protein levels is commonly observed in a broad spectrum of human …

Single-cell RNA sequencing uncovers the nuclear decoy lincRNA PIRAT as a regulator of systemic monocyte immunity during COVID-19

M Aznaourova, N Schmerer, H Janga… - Proceedings of the …, 2022 - National Acad Sciences
The systemic immune response to viral infection is shaped by master transcription factors,
such as NF-κB, STAT1, or PU. 1. Although long noncoding RNAs (lncRNAs) have been …

Cohesin members Stag1 and Stag2 display distinct roles in chromatin accessibility and topological control of HSC self-renewal and differentiation

AD Viny, RL Bowman, Y Liu, VP Lavallée, SE Eisman… - Cell stem cell, 2019 - cell.com
Transcriptional regulators, including the cohesin complex member STAG2, are recurrently
mutated in cancer. The role of STAG2 in gene regulation, hematopoiesis, and tumor …

IL-33-PU. 1 transcriptome reprogramming drives functional state transition and clearance activity of microglia in Alzheimer's disease

SF Lau, C Chen, WY Fu, JY Qu, TH Cheung, AKY Fu… - Cell Reports, 2020 - cell.com
Impairment of microglial clearance activity contributes to beta-amyloid (Aβ) pathology in
Alzheimer's disease (AD). While the transcriptome profile of microglia directs microglial …

Pharmacological restriction of genomic binding sites redirects PU. 1 pioneer transcription factor activity

SJ Taylor, J Stauber, O Bohorquez, G Tatsumi… - Nature Genetics, 2024 - nature.com
Transcription factor (TF) DNA-binding dynamics govern cell fate and identity. However, our
ability to pharmacologically control TF localization is limited. Here we leverage chemically …

Transcriptional, epigenetic and metabolic programming of tumor-associated macrophages

I Larionova, E Kazakova, M Patysheva… - Cancers, 2020 - mdpi.com
Macrophages are key innate immune cells in the tumor microenvironment (TME) that
regulate primary tumor growth, vascularization, metastatic spread and tumor response to …

A novel molecular class that recruits HDAC/MECP2 complexes to PU. 1 motifs reduces neuroinflammation

WT Ralvenius, AE Mungenast, H Woolf… - Journal of Experimental …, 2023 - rupress.org
Pervasive neuroinflammation occurs in many neurodegenerative diseases, including
Alzheimer's disease (AD). SPI1/PU. 1 is a transcription factor located at a genome-wide …