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 …

Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5

KJ Mavrakis, ER McDonald III, MR Schlabach, E Billy… - Science, 2016 - science.org
5-Methylthioadenosine phosphorylase (MTAP) is a key enzyme in the methionine salvage
pathway. The MTAP gene is frequently deleted in human cancers because of its …

The PRMT5 arginine methyltransferase: many roles in development, cancer and beyond

N Stopa, JE Krebs, D Shechter - Cellular and molecular life sciences, 2015 - Springer
Post-translational arginine methylation is responsible for regulation of many biological
processes. The protein arginine methyltransferase 5 (PRMT5, also known as Hsl7, Jbp1 …

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 …

Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers

CR Smith, R Aranda, TP Bobinski… - Journal of Medicinal …, 2022 - ACS Publications
The PRMT5• MTA complex has recently emerged as a new synthetically lethal drug target
for the treatment of MTAP-deleted cancers. Here, we report the discovery of development …

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 …

Targeting arginine methyltransferase PRMT5 for cancer therapy: updated progress and novel strategies

J Zheng, B Li, Y Wu, X Wu, Y Wang - Journal of Medicinal …, 2023 - ACS Publications
As a predominant type II protein arginine methyltransferase, PRMT5 plays critical roles in
various normal cellular processes by catalyzing the mono-and symmetrical dimethylation of …

PRMT5 regulates DNA repair by controlling the alternative splicing of histone-modifying enzymes

PJ Hamard, GE Santiago, F Liu, DL Karl, C Martinez… - Cell reports, 2018 - cell.com
Summary Protein arginine methyltransferase 5 (PRMT5) is overexpressed in many cancer
types and is a promising therapeutic target for several of them, including leukemia and …

A TGFβ-PRMT5-MEP50 axis regulates cancer cell invasion through histone H3 and H4 arginine methylation coupled transcriptional activation and repression

H Chen, B Lorton, V Gupta, D Shechter - Oncogene, 2017 - nature.com
Abstract Protein arginine methyltransferase 5 (PRMT5) complexed with MEP50/WDR77
catalyzes arginine methylation on histones and other proteins. PRMT5-MEP50 activity is …