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

KP Bhat, H Ümit Kaniskan, J **… - 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' …

Role of natural and synthetic compounds in modulating NRF2/KEAP1 signaling pathway in prostate cancer

G Tossetta, S Fantone, D Marzioni, R Mazzucchelli - Cancers, 2023 - mdpi.com
Simple Summary Several studies showed that oxidative stress is involved in cancer
occurrence, development, progression chemoresistance and radio resistance. The nuclear …

Predictive biomarkers of immunotherapy response with pharmacological applications in solid tumors

SA Kovács, JT Fekete, B Győrffy - Acta Pharmacologica Sinica, 2023 - nature.com
Immune-checkpoint inhibitors show promising effects in the treatment of multiple tumor
types. Biomarkers are biological indicators used to select patients for a systemic anticancer …

Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J ** - 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 …

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 …

[HTML][HTML] Mechanistic enzymology in drug discovery: a fresh perspective

GA Holdgate, TD Meek, RL Grimley - Nature reviews Drug discovery, 2018 - nature.com
Given the therapeutic and commercial success of small-molecule enzyme inhibitors, as
exemplified by kinase inhibitors in oncology, a major focus of current drug-discovery and …

A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases

MS Eram, Y Shen, MM Szewczyk, H Wu… - ACS chemical …, 2016 - ACS Publications
Protein arginine methyltransferases (PRMTs) play a crucial role in a variety of biological
processes. Overexpression of PRMTs has been implicated in various human diseases …

The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

Y He, S Selvaraju, ML Curtin, CG Jakob, H Zhu… - Nature chemical …, 2017 - nature.com
Abstract Polycomb repressive complex 2 (PRC2) is a regulator of epigenetic states required
for development and homeostasis. PRC2 trimethylates histone H3 at lysine 27 (H3K27me3) …

Drug discovery targeting nuclear receptor binding SET domain protein 2 (NSD2)

Z Ma, AA Bolinger, H Chen, J Zhou - Journal of medicinal …, 2023 - ACS Publications
Nuclear receptor binding SET domain proteins (NSDs) catalyze the mono-or dimethylation
of histone 3 lysine 36 (H3K36me1 and H3K36me2), using S-adenosyl-l-methionine (SAM) …

The Set7 lysine methyltransferase regulates plasticity in oxidative phosphorylation necessary for trained immunity induced by β-glucan

ST Keating, L Groh, CDCC van der Heijden… - Cell Reports, 2020 - cell.com
Trained immunity confers a sustained augmented response of innate immune cells to a
secondary challenge, via a process dependent on metabolic and transcriptional …