The language of chromatin modification in human cancers

S Zhao, CD Allis, GG Wang - Nature Reviews Cancer, 2021 - nature.com
The genetic information of human cells is stored in the context of chromatin, which is
subjected to DNA methylation and various histone modifications. Such a 'language'of …

Writing, erasing and reading histone lysine methylations

K Hyun, J Jeon, K Park, J Kim - Experimental & molecular medicine, 2017 - nature.com
Histone modifications are key epigenetic regulatory features that have important roles in
many cellular events. Lysine methylations mark various sites on the tail and globular …

MLL-rearranged leukemias—an update on science and clinical approaches

AC Winters, KM Bernt - Frontiers in pediatrics, 2017 - frontiersin.org
The mixed-lineage leukemia 1 (MLL1) gene (now renamed Lysine [K]-specific
MethylTransferase 2A or KMT2A) on chromosome 11q23 is disrupted in a unique group of …

Mll3 and Mll4 facilitate enhancer RNA synthesis and transcription from promoters independently of H3K4 monomethylation

KM Dorighi, T Swigut, T Henriques, NV Bhanu… - Molecular cell, 2017 - cell.com
Monomethylation of histone H3 at lysine 4 (H3K4me1) and acetylation of histone H3 at
lysine 27 (H3K27ac) are correlated with transcriptionally engaged enhancer elements, but …

WD40 repeat domain proteins: a novel target class?

M Schapira, M Tyers, M Torrent… - Nature reviews Drug …, 2017 - nature.com
Antagonism of protein–protein interactions (PPIs) with small molecules is becoming more
feasible as a therapeutic approach. Successful PPI inhibitors tend to target proteins …

An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

W Qi, K Zhao, J Gu, Y Huang, Y Wang, H Zhang… - Nature chemical …, 2017 - nature.com
Abstract Polycomb repressive complex 2 (PRC2) consists of three core subunits, EZH2, EED
and SUZ12, and plays pivotal roles in transcriptional regulation. The catalytic subunit EZH2 …

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 …

Denaturing purifications demonstrate that PRC2 and other widely reported chromatin proteins do not appear to bind directly to RNA in vivo

JK Guo, MR Blanco, WG Walkup, G Bonesteele… - Molecular cell, 2024 - cell.com
Summary Polycomb repressive complex 2 (PRC2) is reported to bind to many RNAs and
has become a central player in reports of how long non-coding RNAs (lncRNAs) regulate …

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 …

Structural basis of nucleosome recognition and modification by MLL methyltransferases

H Xue, T Yao, M Cao, G Zhu, Y Li, G Yuan, Y Chen… - Nature, 2019 - nature.com
Methyltransferases of the mixed-lineage leukaemia (MLL) family—which include MLL1,
MLL2, MLL3, MLL4, SET1A and SET1B—implement methylation of histone H3 on lysine 4 …