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 …

[HTML][HTML] Protein arginine methyltransferase 3: A crucial regulator in metabolic reprogramming and gene expression in cancers

SH Hsu, WC Hung - Cancer letters, 2023 - Elsevier
Post-translational modification (PTM) of proteins increases proteome diversity, which is
critical for maintaining cellular homeostasis. The importance of protein methylation in the …

Allosteric modulator discovery: from serendipity to structure-based design

S Lu, X He, D Ni, J Zhang - Journal of medicinal chemistry, 2019 - ACS Publications
Allosteric modulators bound to structurally diverse allosteric sites can achieve better
pharmacological advantages than orthosteric ligands. The discovery of allosteric …

Identification and inhibition of the druggable allosteric site of SARS-CoV-2 NSP10/NSP16 methyltransferase through computational approaches

S Faisal, SL Badshah, B Kubra, M Sharaf, AH Emwas… - Molecules, 2022 - mdpi.com
Since its emergence in early 2019, the respiratory infectious virus, SARS-CoV-2, has
ravaged the health of millions of people globally and has affected almost every sphere of …

Allosteric modulation of protein arginine methyltransferase 5 (PRMT5)

RL Palte, SE Schneider, MD Altman… - ACS Medicinal …, 2020 - ACS Publications
Protein arginine methyltransferase 5 (PRMT5) belongs to a family of enzymes that regulate
the posttranslational modification of histones and other proteins via methylation of arginine …

Non-histone arginine methylation by protein arginine methyltransferases

AA Al-Hamashi, K Diaz, R Huang - Current Protein and Peptide …, 2020 - ingentaconnect.com
Protein arginine methyltransferase (PRMT) enzymes play a crucial role in RNA splicing,
DNA damage repair, cell signaling, and differentiation. Arginine methylation is a prominent …

Targeting epigenetic regulation for cancer therapy using small molecule inhibitors

A Kumar, L Emdad, PB Fisher, SK Das - Advances in Cancer Research, 2023 - Elsevier
Cancer cells display pervasive changes in DNA methylation, disrupted patterns of histone
posttranslational modification, chromatin composition or organization and regulatory …

Methyltransferase inhibitors: competing with, or exploiting the bound cofactor

R Ferreira de Freitas, D Ivanochko, M Schapira - Molecules, 2019 - mdpi.com
Protein methyltransferases (PMTs) are enzymes involved in epigenetic mechanisms, DNA
repair, and other cellular machineries critical to cellular identity and function, and are an …

Discovery of a first-in-class protein arginine methyltransferase 6 (PRMT6) covalent inhibitor

Y Shen, F Li, MM Szewczyk, L Halabelian… - Journal of medicinal …, 2020 - ACS Publications
Protein arginine methyltransferase 6 (PRMT6) plays important roles in several biological
processes associated with multiple cancers. Well-characterized potent, selective, and cell …

The methylation status of the epigenome: its emerging role in the regulation of tumor angiogenesis and tumor growth, and potential for drug targeting

L Pirola, O Ciesielski, A Balcerczyk - Cancers, 2018 - mdpi.com
Approximately 50 years ago, Judah Folkman raised the concept of inhibiting tumor
angiogenesis for treating solid tumors. The development of anti-angiogenic drugs would …