Bromodomains: a new target class for drug development

AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

[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 …

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 …

Beyond histone acetylation—writing and erasing histone acylations

S Zhao, X Zhang, H Li - Current opinion in structural biology, 2018 - Elsevier
Highlights•Non-acetyl histone acylations are catalyzed by classical acetylation
modifiers.•Active site engagement of the acyl group determines acyl type-specific …

Structural mechanism of BRD4-NUT and p300 bipartite interaction in propagating aberrant gene transcription in chromatin in NUT carcinoma

D Yu, Y Liang, C Kim, A Jaganathan, D Ji… - Nature …, 2023 - nature.com
BRD4-NUT, a driver fusion mutant in rare and highly aggressive NUT carcinoma, acts in
aberrant transcription of anti-differentiation genes by recruiting histone acetyltransferase …

The role of CREBBP/EP300 and its therapeutic implications in hematological malignancies

Y Zhu, Z Wang, Y Li, H Peng, J Liu, J Zhang, X Xiao - Cancers, 2023 - mdpi.com
Simple Summary Through their regulatory effects on gene expression, histone
acetyltransferases have been implicated in the normal physiological activities and genesis …

Dynamics of histone acetylation during human early embryogenesis

K Wu, D Fan, H Zhao, Z Liu, Z Hou, W Tao, G Yu… - Cell Discovery, 2023 - nature.com
It remains poorly understood about the regulation of gene and transposon transcription
during human early embryogenesis. Here, we report that broad H3K27ac domains are …

Epigenetic mechanisms to propagate histone acetylation by p300/CBP

M Kikuchi, S Morita, M Wakamori, S Sato… - Nature …, 2023 - nature.com
Histone acetylation is important for the activation of gene transcription but little is known
about its direct read/write mechanisms. Here, we report cryogenic electron microscopy …

EP300 as a molecular integrator of fibrotic transcriptional programs

K Rubio, A Molina-Herrera, A Pérez-González… - International Journal of …, 2023 - mdpi.com
Fibrosis is a condition characterized by the excessive accumulation of extracellular matrix
proteins in tissues, leading to organ dysfunction and failure. Recent studies have identified …

p300 is an obligate integrator of combinatorial transcription factor inputs

JJ Ferrie, JP Karr, TGW Graham, GM Dailey, G Zhang… - Molecular Cell, 2024 - cell.com
Transcription coactivators are proteins or protein complexes that mediate transcription factor
(TF) function. However, they lack DNA-binding capacity, prompting the question of how they …