Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …

Chemoenzymatic semisynthesis of proteins

RE Thompson, TW Muir - Chemical reviews, 2019 - ACS Publications
Protein semisynthesis—defined herein as the assembly of a protein from a combination of
synthetic and recombinant fragments—is a burgeoning field of chemical biology that has …

PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS

JL Dahlin, JWM Nissink, JM Strasser… - Journal of medicinal …, 2015 - ACS Publications
Significant resources in early drug discovery are spent unknowingly pursuing artifacts and
promiscuous bioactive compounds, while understanding the chemical basis for these …

Current development of CBP/p300 inhibitors in the last decade

ZX He, BF Wei, X Zhang, YP Gong, LY Ma… - European Journal of …, 2021 - Elsevier
CBP/p300, functioning as histone acetyltransferases and transcriptional co-factors,
represents an attractive target for various diseases, including malignant tumor. The …

Acetyl-CoA biosynthesis drives resistance to histone acetyltransferase inhibition

TR Bishop, C Subramanian, EM Bilotta… - Nature chemical …, 2023 - nature.com
Histone acetyltransferases (HATs) are implicated as both oncogene and nononcogene
dependencies in diverse human cancers. Acetyl-CoA-competitive HAT inhibitors have …

Alzheimer's disease-related epigenetic changes: novel therapeutic targets

A Paniri, MM Hosseini, H Akhavan-Niaki - Molecular Neurobiology, 2024 - Springer
Aging is a significant risk factor for Alzheimer's disease (AD), although the precise
mechanism and molecular basis of AD are not yet fully understood. Epigenetic mechanisms …

[HTML][HTML] Acetyltransferases (HATs) as targets for neurological therapeutics

A Schneider, S Chatterjee, O Bousiges, BR Selvi… - …, 2013 - Elsevier
The acetylation of histone and non-histone proteins controls a great deal of cellular
functions, thereby affecting the entire organism, including the brain. Acetylation …

Genetically encoded system to track histone modification in vivo

Y Sato, M Mukai, J Ueda, M Muraki, TJ Stasevich… - Scientific reports, 2013 - nature.com
Post-translational histone modifications play key roles in gene regulation, development and
differentiation, but their dynamics in living organisms remain almost completely unknown. To …

CBP regulates recruitment and release of promoter-proximal RNA polymerase II

A Boija, DB Mahat, A Zare, PH Holmqvist, P Philip… - Molecular cell, 2017 - cell.com
Transcription activation involves RNA polymerase II (Pol II) recruitment and release from the
promoter into productive elongation, but how specific chromatin regulators control these …

[HTML][HTML] Histone/protein deacetylase inhibitor therapy for enhancement of Foxp3+ T-regulatory cell function posttransplantation

L Wang, UH Beier, T Akimova, S Dahiya, R Han… - American Journal of …, 2018 - Elsevier
T-regulatory (Treg) cells are like other cells present throughout the body in being subject to
biochemical modifications in response to extracellular signals. An important component of …