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' …

YTH Domain: A Family of N6-Methyladenosine (m6A) Readers

S Liao, H Sun, C Xu - Genomics, Proteomics and Bioinformatics, 2018 - academic.oup.com
Like protein and DNA, different types of RNA molecules undergo various modifications.
Accumulating evidence suggests that these RNA modifications serve as sophisticated codes …

Nuclear condensates of the Polycomb protein chromobox 2 (CBX2) assemble through phase separation

R Tatavosian, S Kent, K Brown, T Yao, HN Duc… - Journal of Biological …, 2019 - ASBMB
Polycomb group (PcG) proteins repress master regulators of development and differentiation
through organization of chromatin structure. Mutation and dysregulation of PcG genes cause …

Inhibition of PRC2 activity by a gain-of-function H3 mutation found in pediatric glioblastoma

PW Lewis, MM Müller, MS Koletsky, F Cordero, S Lin… - Science, 2013 - science.org
Sequencing of pediatric gliomas has identified missense mutations Lys27Met (K27M) and
Gly34Arg/Val (G34R/V) in genes encoding histone H3. 3 (H3F3A) and H3. 1 (HIST3H1B) …

Perceiving the epigenetic landscape through histone readers

CA Musselman, ME Lalonde, J Côté… - Nature structural & …, 2012 - nature.com
Post-translational modifications (PTMs) of histones provide a fine-tuned mechanism for
regulating chromatin structure and dynamics. PTMs can alter direct interactions between …

Regulation of gene transcription by Polycomb proteins

S Aranda, G Mas, L Di Croce - Science advances, 2015 - science.org
The Polycomb group (PcG) of proteins defines a subset of factors that physically associate
and function to maintain the positional identity of cells from the embryo to adult stages. PcG …

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

SK Knutson, TJ Wigle, NM Warholic… - Nature chemical …, 2012 - nature.com
EZH2 catalyzes trimethylation of histone H3 lysine 27 (H3K27). Point mutations of EZH2 at
Tyr641 and Ala677 occur in subpopulations of non-Hodgkin's lymphoma, where they drive …

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 …

[HTML][HTML] Occupying chromatin: Polycomb mechanisms for getting to genomic targets, stopping transcriptional traffic, and staying put

JA Simon, RE Kingston - Molecular cell, 2013 - cell.com
Chromatin modification by Polycomb proteins provides an essential strategy for gene
silencing in higher eukaryotes. Polycomb repressive complexes (PRCs) silence key …

Polycomb and Trithorax Group Genes in Drosophila

JA Kassis, JA Kennison, JW Tamkun - Genetics, 2017 - academic.oup.com
Abstract Polycomb group (PcG) and Trithorax group (TrxG) genes encode important
regulators of development and differentiation in metazoans. These two groups of genes …