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 …

[HTML][HTML] Roles of H3K4 methylation in biology and disease

H Wang, K Helin - Trends in Cell Biology, 2024 - cell.com
Epigenetic modifications, including posttranslational modifications of histones, are closely
linked to transcriptional regulation. Trimethylated H3 lysine 4 (H3K4me3) is one of the most …

Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

DE Scott, AR Bayly, C Abell, J Skidmore - Nature Reviews Drug …, 2016 - nature.com
Protein–protein interactions (PPIs) are of pivotal importance in the regulation of biological
systems and are consequently implicated in the development of disease states. Recent work …

Targeting transcription factors for cancer treatment

M Lambert, S Jambon, S Depauw… - Molecules, 2018 - mdpi.com
Transcription factors are involved in a large number of human diseases such as cancers for
which they account for about 20% of all oncogenes identified so far. For long time, with the …

N6-methyladenosine RNA modification regulates embryonic neural stem cell self-renewal through histone modifications

Y Wang, Y Li, M Yue, J Wang, S Kumar… - Nature …, 2018 - nature.com
Abstract Internal N 6-methyladenosine (m6A) modification is widespread in messenger
RNAs (mRNAs) and is catalyzed by heterodimers of methyltransferase-like protein 3 (Mettl3) …

Targeting transcription cycles in cancer

SJ Vervoort, JR Devlin, N Kwiatkowski, M Teng… - Nature Reviews …, 2022 - nature.com
Accurate control of gene expression is essential for normal development and dysregulation
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …

Hijacked in cancer: the KMT2 (MLL) family of methyltransferases

RC Rao, Y Dou - Nature Reviews Cancer, 2015 - nature.com
Abstract Histone–lysine N-methyltransferase 2 (KMT2) family proteins methylate lysine 4 on
the histone H3 tail at important regulatory regions in the genome and thereby impart crucial …

A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models

X Yu, D Li, J Kottur, Y Shen, HS Kim, KS Park… - Science translational …, 2021 - science.org
Interactions between WD40 repeat domain protein 5 (WDR5) and its various partners such
as mixed lineage leukemia (MLL) and c-MYC are essential for sustaining oncogenesis in …

Rational design of peptide-based inhibitors disrupting protein-protein interactions

X Wang, D Ni, Y Liu, S Lu - Frontiers in chemistry, 2021 - frontiersin.org
Protein-protein interactions (PPIs) are well-established as a class of promising drug targets
for their implications in a wide range of biological processes. However, drug development …

Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth

J Zhu, MA Sammons, G Donahue, Z Dou, M Vedadi… - Nature, 2015 - nature.com
TP53 (which encodes p53 protein) is the most frequently mutated gene among all human
cancers. Prevalent p53 missense mutations abrogate its tumour suppressive function and …