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Writing, erasing and reading histone lysine methylations
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 …
many cellular events. Lysine methylations mark various sites on the tail and globular …
[HTML][HTML] Roles of H3K4 methylation in biology and disease
Epigenetic modifications, including posttranslational modifications of histones, are closely
linked to transcriptional regulation. Trimethylated H3 lysine 4 (H3K4me3) is one of the most …
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 …
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 …
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
Abstract Internal N 6-methyladenosine (m6A) modification is widespread in messenger
RNAs (mRNAs) and is catalyzed by heterodimers of methyltransferase-like protein 3 (Mettl3) …
RNAs (mRNAs) and is catalyzed by heterodimers of methyltransferase-like protein 3 (Mettl3) …
Targeting transcription cycles in cancer
Accurate control of gene expression is essential for normal development and dysregulation
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …
Hijacked in cancer: the KMT2 (MLL) family of methyltransferases
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 …
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
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 …
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 …
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
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 …
cancers. Prevalent p53 missense mutations abrogate its tumour suppressive function and …