Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease

KP Bhat, H Ümit Kaniskan, J Jin… - Nature Reviews Drug …, 2021 - nature.com
Protein lysine methylation is a crucial post-translational modification that regulates the
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …

Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J Jin - Chemical reviews, 2018 - ACS Publications
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

[HTML][HTML] Chemical-induced chromatin remodeling reprograms mouse ESCs to totipotent-like stem cells

M Yang, H Yu, X Yu, S Liang, Y Hu, Y Luo, Z Izsvák… - Cell Stem Cell, 2022 - cell.com
Totipotent cells have more robust developmental potency than any other cell types, giving
rise to both embryonic and extraembryonic tissues. Stable totipotent cell cultures and …

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

LM Lasko, CG Jakob, RP Edalji, W Qiu, D Montgomery… - Nature, 2017 - nature.com
The dynamic and reversible acetylation of proteins, catalysed by histone acetyltransferases
(HATs) and histone deacetylases (HDACs), is a major epigenetic regulatory mechanism of …

Chemical and biochemical perspectives of protein lysine methylation

M Luo - Chemical reviews, 2018 - ACS Publications
Protein lysine methylation is a distinct posttranslational modification that causes minimal
changes in the size and electrostatic status of lysine residues. Lysine methylation plays …

DNMT1 reads heterochromatic H4K20me3 to reinforce LINE-1 DNA methylation

W Ren, H Fan, SA Grimm, JJ Kim, L Li, Y Guo… - Nature …, 2021 - nature.com
DNA methylation and trimethylated histone H4 Lysine 20 (H4K20me3) constitute two
important heterochromatin-enriched marks that frequently cooperate in silencing repetitive …

TGF-β signaling alters H4K20me3 status via miR-29 and contributes to cellular senescence and cardiac aging

G Lyu, Y Guan, C Zhang, L Zong, L Sun… - Nature …, 2018 - nature.com
Cellular senescence is a well-orchestrated programmed process involved in age-related
pathologies, tumor suppression and embryonic development. TGF-β/Smad is one of the …

The chromatin response to double-strand DNA breaks and their repair

R Aleksandrov, R Hristova, S Stoynov, A Gospodinov - Cells, 2020 - mdpi.com
Cellular DNA is constantly being damaged by numerous internal and external mutagenic
factors. Probably the most severe type of insults DNA could suffer are the double-strand …

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling

S Scheer, S Ackloo, TS Medina, M Schapira, F Li… - Nature …, 2019 - nature.com
Protein methyltransferases (PMTs) comprise a major class of epigenetic regulatory enzymes
with therapeutic relevance. Here we present a collection of chemical probes and associated …

Replication-coupled dilution of H4K20me2 guides 53BP1 to pre-replicative chromatin

S Pellegrino, J Michelena, F Teloni, R Imhof… - Cell reports, 2017 - cell.com
The bivalent histone modification reader 53BP1 accumulates around DNA double-strand
breaks (DSBs), where it dictates repair pathway choice decisions by limiting DNA end …