Inhibitors of protein methyltransferases and demethylases
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …
histone demethylases (KDMs) play an important role in the regulation of gene expression …
The emerging role of PRMT6 in cancer
Z Chen, J Gan, Z Wei, M Zhang, Y Du, C Xu… - Frontiers in …, 2022 - frontiersin.org
Protein arginine methyltransferase 6 (PRMT6) is a type I PRMT that is involved in epigenetic
regulation of gene expression through methylating histone or non-histone proteins, and …
regulation of gene expression through methylating histone or non-histone proteins, and …
A patent review of arginine methyltransferase inhibitors (2010–2018)
ABSTRACT Introduction: Protein arginine methyltransferases (PRMTs) are fundamental
enzymes that specifically modify the arginine residues of versatile substrates in cells. The …
enzymes that specifically modify the arginine residues of versatile substrates in cells. The …
[HTML][HTML] TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma
K Nakayama, MM Szewczyk, C dela Sena, H Wu… - Oncotarget, 2018 - ncbi.nlm.nih.gov
Abstract Protein arginine methyltransferase (PRMT) 4 (also known as coactivator-associated
arginine methyltransferase 1; CARM1) is involved in a variety of biological processes and is …
arginine methyltransferase 1; CARM1) is involved in a variety of biological processes and is …
Targeting histone methylation in cancer
MT McCabe, HP Mohammad, O Barbash… - The Cancer …, 2017 - journals.lww.com
Most, if not all, human cancers exhibit altered epigenetic signatures that promote aberrant
gene expression that contributes to cellular transformation. Historically, attempts to …
gene expression that contributes to cellular transformation. Historically, attempts to …
Overview of PRMT1 modulators: Inhibitors and degraders
J Wu, D Li, L Wang - European Journal of Medicinal Chemistry, 2024 - Elsevier
Abstract Protein arginine methyltransferase 1 (PRMT1) is pivotal in executing normal cellular
functions through its catalytic action on the methylation of arginine side chains on protein …
functions through its catalytic action on the methylation of arginine side chains on protein …
Discovery of a potent, selective, and cell-active dual inhibitor of protein arginine methyltransferase 4 and protein arginine methyltransferase 6
Well-characterized selective inhibitors of protein arginine methyltransferases (PRMTs) are
invaluable chemical tools for testing biological and therapeutic hypotheses. Based on 4, a …
invaluable chemical tools for testing biological and therapeutic hypotheses. Based on 4, a …
Epigenetic control via allosteric regulation of mammalian protein arginine methyltransferases
Arginine methylation on histones is a central player in epigenetics and in gene activation
and repression. Protein arginine methyltransferase (PRMT) activity has been implicated in …
and repression. Protein arginine methyltransferase (PRMT) activity has been implicated in …
Targeting epigenetic regulators with covalent small-molecule inhibitors
Y Zhang, D Rong, B Li, Y Wang - Journal of Medicinal Chemistry, 2021 - ACS Publications
Epigenetic regulation of gene expression plays a critical role in various physiological
processes, and epigenetic dysregulation is implicated in a number of diseases, prominently …
processes, and epigenetic dysregulation is implicated in a number of diseases, prominently …
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 …
processes associated with multiple cancers. Well-characterized potent, selective, and cell …