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 …

Eukaryotic core promoters and the functional basis of transcription initiation

V Haberle, A Stark - Nature reviews Molecular cell biology, 2018 - nature.com
Abstract RNA polymerase II (Pol II) core promoters are specialized DNA sequences at
transcription start sites of protein-coding and non-coding genes that support the assembly of …

BRD4 and Cancer: going beyond transcriptional regulation

B Donati, E Lorenzini, A Ciarrocchi - Molecular cancer, 2018 - Springer
BRD4, member of the Bromodomain and Extraterminal (BET) protein family, is largely
acknowledged in cancer for its role in super-enhancers (SEs) organization and oncogenes …

[HTML][HTML] Nrf2 suppresses macrophage inflammatory response by blocking proinflammatory cytokine transcription

EH Kobayashi, T Suzuki, R Funayama… - Nature …, 2016 - nature.com
Abstract Nrf2 (NF-E2-related factor-2) transcription factor regulates oxidative/xenobiotic
stress response and also represses inflammation. However, the mechanisms how Nrf2 …

[HTML][HTML] Histone acetyltransferases CBP/p300 in tumorigenesis and CBP/p300 inhibitors as promising novel anticancer agents

Q Chen, B Yang, X Liu, XD Zhang, L Zhang, T Liu - Theranostics, 2022 - ncbi.nlm.nih.gov
The histone acetyltransferases CBP and p300, often referred to as CBP/p300 due to their
sequence homology and functional overlap and co-operation, are emerging as critical …

Massively multiplex chemical transcriptomics at single-cell resolution

SR Srivatsan, JL McFaline-Figueroa, V Ramani… - Science, 2020 - science.org
High-throughput chemical screens typically use coarse assays such as cell survival, limiting
what can be learned about mechanisms of action, off-target effects, and heterogeneous …

BET proteins as targets for anticancer treatment

A Stathis, F Bertoni - Cancer discovery, 2018 - AACR
Bromodomain and extraterminal domain (BET) proteins are epigenetic readers that regulate
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …

Protein acylation: mechanisms, biological functions and therapeutic targets

S Shang, J Liu, F Hua - Signal Transduction and Targeted Therapy, 2022 - nature.com
Metabolic reprogramming is involved in the pathogenesis of not only cancers but also
neurodegenerative diseases, cardiovascular diseases, and infectious diseases. With the …

In vivo CD8+ T cell CRISPR screening reveals control by Fli1 in infection and cancer

Z Chen, E Arai, O Khan, Z Zhang, SF Ngiow, Y He… - Cell, 2021 - cell.com
Improving effector activity of antigen-specific T cells is a major goal in cancer
immunotherapy. Despite the identification of several effector T cell (T EFF)-driving …

Lysine acetylation goes global: from epigenetics to metabolism and therapeutics

I Ali, RJ Conrad, E Verdin, M Ott - Chemical reviews, 2018 - ACS Publications
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …