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 …

Quantitative proteomic analysis of histone modifications

H Huang, S Lin, BA Garcia, Y Zhao - Chemical reviews, 2015 - ACS Publications
Several mechanisms have been proposed for histone marks to exert their functions,
including altering the physical properties of nucleosomes by neutralization of charge via …

Regulation of the Dot1 histone H3K79 methyltransferase by histone H4K16 acetylation

MI Valencia-Sánchez, P De Ioannes, M Wang… - Science, 2021 - science.org
INTRODUCTION Nucleosomes—the primary, repeating unit of chromatin—package and
protect the genome while also transmitting various regulatory signals through, in part …

The diverse functions of Dot1 and H3K79 methylation

AT Nguyen, Y Zhang - Genes & development, 2011 - genesdev.cshlp.org
DOT1 (disruptor of telomeric silencing; also called Kmt4) was initially discovered in budding
yeast in a genetic screen for genes whose deletion confers defects in telomeric silencing …

DOT1L and H3K79 methylation in transcription and genomic stability

K Wood, M Tellier, S Murphy - Biomolecules, 2018 - mdpi.com
The organization of eukaryotic genomes into chromatin provides challenges for the cell to
accomplish basic cellular functions, such as transcription, DNA replication and repair of DNA …

Protein methyltransferases as a target class for drug discovery

RA Copeland, ME Solomon, VM Richon - Nature reviews Drug …, 2009 - nature.com
The protein methyltransferases (PMTs)—which methylate protein lysine and arginine
residues and have crucial roles in gene transcription—are emerging as an important group …

Histone methyltransferase DOT1L coordinates AR and MYC stability in prostate cancer

R Vatapalli, V Sagar, Y Rodriguez, JC Zhao… - Nature …, 2020 - nature.com
The histone methyltransferase DOT1L methylates lysine 79 (K79) on histone H3 and is
involved in Mixed Lineage Leukemia (MLL) fusion leukemogenesis; however, its role in …

Sound of silence: the properties and functions of repressive Lys methyltransferases

C Mozzetta, E Boyarchuk, J Pontis… - Nature Reviews Molecular …, 2015 - nature.com
The methylation of histone Lys residues by Lys methyltransferases (KMTs) regulates
chromatin organization and either activates or represses gene expression, depending on …

Transcription-associated histone modifications and cryptic transcription

M Smolle, JL Workman - Biochimica et Biophysica Acta (BBA)-Gene …, 2013 - Elsevier
Eukaryotic genomes are packaged into chromatin, a highly organized structure consisting of
DNA and histone proteins. All nuclear processes take place in the context of chromatin …

Histone modification patterns and epigenetic codes

A Lennartsson, K Ekwall - Biochimica et biophysica acta (BBA)-general …, 2009 - Elsevier
The eukaryotic DNA is wrapped around histone octamers, which consist of four different
histones, H2A, H2B, H3 and H4. The N-terminal tail of each histone is post-transcriptionally …