Histone modifications and cancer

JE Audia, RM Campbell - Cold Spring Harbor …, 2016 - cshperspectives.cshlp.org
Histone posttranslational modifications represent a versatile set of epigenetic marks
involved not only in dynamic cellular processes, such as transcription and DNA repair, but …

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 …

Iterative design and optimization of initially inactive proteolysis targeting chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von Hippel–Lindau (VHL) …

V Zoppi, SJ Hughes, C Maniaci, A Testa… - Journal of medicinal …, 2018 - ACS Publications
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently
degrade a target protein within cells can be a lengthy and unpredictable process, and it …

Cancer genetics and epigenetics: two sides of the same coin?

JS You, PA Jones - Cancer cell, 2012 - cell.com
Epigenetic and genetic alterations have long been thought of as two separate mechanisms
participating in carcinogenesis. A recent outcome of whole exome sequencing of thousands …

SWI/SNF nucleosome remodellers and cancer

BG Wilson, CWM Roberts - Nature Reviews Cancer, 2011 - nature.com
SWI/SNF chromatin remodelling complexes use the energy of ATP hydrolysis to remodel
nucleosomes and to modulate transcription. Growing evidence indicates that these …

Increased global transcription activity as a mechanism of replication stress in cancer

P Kotsantis, LM Silva, S Irmscher, RM Jones… - Nature …, 2016 - nature.com
Cancer is a disease associated with genomic instability that often results from oncogene
activation. This in turn leads to hyperproliferation and replication stress. However, the …

ATP-dependent chromatin remodeling: genetics, genomics and mechanisms

DC Hargreaves, GR Crabtree - Cell research, 2011 - nature.com
Macromolecular assemblies that regulate chromatin structure using the energy of ATP
hydrolysis have critical roles in development, cancer, and stem cell biology. The ATPases of …

Functional genetic screens for enhancer elements in the human genome using CRISPR-Cas9

G Korkmaz, R Lopes, AP Ugalde… - Nature …, 2016 - nature.com
Systematic identification of noncoding regulatory elements has, to date, mainly relied on
large-scale reporter assays that do not reproduce endogenous conditions. We present two …

[HTML][HTML] eRNAs are required for p53-dependent enhancer activity and gene transcription

CA Melo, J Drost, PJ Wijchers, H van de Werken… - Molecular cell, 2013 - cell.com
Binding within or nearby target genes involved in cell proliferation and survival enables the
p53 tumor suppressor gene to regulate their transcription and cell-cycle progression. Using …

[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology

CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …