Protein arginine methylation: from enigmatic functions to therapeutic targeting

Q Wu, M Schapira, CH Arrowsmith… - Nature reviews Drug …, 2021 - nature.com
Protein arginine methyltransferases (PRMTs) are emerging as attractive therapeutic targets.
PRMTs regulate transcription, splicing, RNA biology, the DNA damage response and cell …

Protein arginine methyltransferases: promising targets for cancer therapy

JW Hwang, Y Cho, GU Bae, SN Kim… - Experimental & molecular …, 2021 - nature.com
Protein methylation, a post-translational modification (PTM), is observed in a wide variety of
cell types from prokaryotes to eukaryotes. With recent and rapid advancements in epigenetic …

MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer

LD Engstrom, R Aranda, L Waters, K Moya, V Bowcut… - Cancer discovery, 2023 - AACR
Previous studies implicated protein arginine methyltransferase 5 (PRMT5) as a synthetic
lethal target for MTAP-deleted (MTAP del) cancers; however, the pharmacologic …

DNA hypermethylation in disease: mechanisms and clinical relevance

M Ehrlich - Epigenetics, 2019 - Taylor & Francis
Increasing numbers of studies implicate abnormal DNA methylation in cancer and many non-
malignant diseases. This is consistent with numerous findings about differentiation …

[HTML][HTML] Arginine methylation: the coming of age

RS Blanc, S Richard - Molecular cell, 2017 - cell.com
Arginine methylation is a common post-translational modification functioning as an
epigenetic regulator of transcription and playing key roles in pre-mRNA splicing, DNA …

Cellular pathways influenced by protein arginine methylation: Implications for cancer

J Xu, S Richard - Molecular cell, 2021 - cell.com
Arginine methylation is an influential post-translational modification occurring on histones,
RNA binding proteins, and many other cellular proteins, affecting their function by altering …

[HTML][HTML] PRMT5 function and targeting in cancer

H Kim, AR Ze'ev - Cell stress, 2020 - ncbi.nlm.nih.gov
Protein methyl transferases play critical roles in numerous regulatory pathways that underlie
cancer development, progression and therapy-response. Here we discuss the function of …

PRMTs and arginine methylation: cancer's best-kept secret?

J Jarrold, CC Davies - Trends in molecular medicine, 2019 - cell.com
Post-translational modification (PTM) of proteins is vital for increasing proteome diversity
and maintaining cellular homeostasis. If the writing, reading, and removal of modifications …

The mechanisms behind the therapeutic activity of BET bromodomain inhibition

J Shi, CR Vakoc - Molecular cell, 2014 - cell.com
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …

Methyl-CpG-binding domain proteins: readers of the epigenome

Q Du, PL Luu, C Stirzaker, SJ Clark - Epigenomics, 2015 - Taylor & Francis
How DNA methylation is interpreted and influences genome regulation remains largely
unknown. Proteins of the methyl-CpG-binding domain (MBD) family are primary candidates …