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 …

Toxic dimethylarginines: asymmetric dimethylarginine (ADMA) and symmetric dimethylarginine (SDMA)

YL Tain, CN Hsu - Toxins, 2017 - mdpi.com
Asymmetric and symmetric dimethylarginine (ADMA and SDMA, respectively) are toxic, non-
proteinogenic amino acids formed by post-translational modification and are uremic toxins …

Profiling PRMT methylome reveals roles of hnRNPA1 arginine methylation in RNA splicing and cell growth

W Li, Y He, J Yang, G Hu, Y Lin, T Ran, B Peng… - Nature …, 2021 - nature.com
Numerous substrates have been identified for Type I and II arginine methyltransferases
(PRMTs). However, the full substrate spectrum of the only type III PRMT, PRMT7, and its …

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 …

The protein arginine methyltransferase PRMT9 attenuates MAVS activation through arginine methylation

X Bai, C Sui, F Liu, T Chen, L Zhang, Y Zheng… - Nature …, 2022 - nature.com
The signaling adaptor MAVS forms prion-like aggregates to activate the innate antiviral
immune response after viral infection. However, spontaneous aggregation of MAVS can …

LLY-283, a potent and selective inhibitor of arginine methyltransferase 5, PRMT5, with antitumor activity

ZQ Bonday, GS Cortez, MJ Grogan… - ACS medicinal …, 2018 - ACS Publications
Protein arginine methyltransferase 5 (PRMT5) is a type II arginine methyltransferase that
catalyzes the formation of symmetric dimethylarginine in a number of nuclear and …

PRMT1 methylation of WTAP promotes multiple myeloma tumorigenesis by activating oxidative phosphorylation via m6A modification of NDUFS6

Y Jia, X Yu, R Liu, L Shi, H Jin, D Yang, X Zhang… - Cell Death & …, 2023 - nature.com
Epigenetic modifications play important roles during the pathogenesis of multiple myeloma
(MM). Herein, we found that protein arginine methyltransferase 1 (PRMT1) was highly …

Epidrug repurposing: discovering new faces of old acquaintances in cancer therapy

M Montalvo-Casimiro, R González-Barrios… - Frontiers in …, 2020 - frontiersin.org
Gene mutations are strongly associated with tumor progression and are well known in
cancer development. However, recently discovered epigenetic alterations have shown the …

Protein arginine methyltransferases: insights into the enzyme structure and mechanism at the atomic level

SK Tewary, YG Zheng, MC Ho - Cellular and Molecular Life Sciences, 2019 - Springer
Protein arginine methyltransferases (PRMTs) catalyze the methyl transfer to the arginine
residues of protein substrates and are classified into three major types based on the final …

Structure, activity, and function of PRMT1

C Thiebaut, L Eve, C Poulard, M Le Romancer - Life, 2021 - mdpi.com
PRMT1, the major protein arginine methyltransferase in mammals, catalyzes
monomethylation and asymmetric dimethylation of arginine side chains in proteins. Initially …