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 …

The regulation, functions and clinical relevance of arginine methylation

E Guccione, S Richard - Nature reviews Molecular cell biology, 2019 - nature.com
Methylation of arginine residues by protein arginine methyltransferases (PRMTs) is involved
in the regulation of fundamental cellular processes, including transcription, RNA processing …

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 …

Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

HP Mohammad, O Barbash, CL Creasy - Nature medicine, 2019 - nature.com
Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

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 …

Methionine is a metabolic dependency of tumor-initiating cells

Z Wang, LY Yip, JHJ Lee, Z Wu, HY Chew… - Nature medicine, 2019 - nature.com
Understanding cellular metabolism holds immense potential for developing new classes of
therapeutics that target metabolic pathways in cancer. Metabolic pathways are altered in …

[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 …

Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP loss

A Fedoriw, SR Rajapurkar, S O'Brien, SV Gerhart… - Cancer cell, 2019 - cell.com
Type I protein arginine methyltransferases (PRMTs) catalyze asymmetric dimethylation of
arginines on proteins. Type I PRMTs and their substrates have been implicated in human …