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 …

SAM/SAH analogs as versatile tools for SAM-dependent methyltransferases

J Zhang, YG Zheng - ACS chemical biology, 2016 - ACS Publications
S-Adenosyl-L-methionine (SAM) is a sulfonium molecule with a structural hybrid of
methionine and adenosine. As the second largest cofactor in the human body, its major …

Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment

M Schwickert, TR Fischer… - Journal of Medicinal …, 2022 - ACS Publications
Selective manipulation of the epitranscriptome could be beneficial for the treatment of
cancer and also broaden the understanding of epigenetic inheritance. Inhibitors of the tRNA …

Discovery of novel substrate-competitive lysine methyltransferase G9a inhibitors as anticancer agents

Y Nishigaya, S Takase, T Sumiya… - Journal of Medicinal …, 2023 - ACS Publications
Identification of structurally novel inhibitors of lysine methyltransferase G9a has been a
subject of intense research in cancer epigenetics. Starting with the high-throughput …

Discovery of potent and selective inhibitors for G9a-like protein (GLP) lysine methyltransferase

Y Xiong, F Li, N Babault, A Dong, H Zeng… - Journal of medicinal …, 2017 - ACS Publications
G9a-like protein (GLP) and G9a are highly homologous protein lysine methyltransferases
(PKMTs) sharing approximately 80% sequence identity in their catalytic domains. GLP and …

[HTML][HTML] Lysine methyltransferase inhibitors: where we are now

A Feoli, M Viviano, A Cipriano, C Milite… - RSC Chemical …, 2022 - pubs.rsc.org
Protein lysine methyltransferases constitute a large family of epigenetic writers that catalyse
the transfer of a methyl group from the cofactor S-adenosyl-L-methionine to histone-and non …

[HTML][HTML] Benzoxaborole treatment perturbs S-adenosyl-L-methionine metabolism in Trypanosoma brucei

PC Steketee, IM Vincent, F Achcar… - PLoS neglected …, 2018 - journals.plos.org
The parasitic protozoan Trypanosoma brucei causes Human African Trypanosomiasis and
Nagana in other mammals. These diseases present a major socio-economic burden to large …

Discovery of a novel chemotype of histone lysine methyltransferase EHMT1/2 (GLP/G9a) inhibitors: rational design, synthesis, biological evaluation, and co-crystal …

C Milite, A Feoli, JR Horton, D Rescigno… - Journal of medicinal …, 2019 - ACS Publications
Since the discovery of compound BIX01294 over 10 years ago, only a very limited number of
nonquinazoline inhibitors of H3K9-specific methyltransferases G9a and G9a-like protein …

Structure-based design and characterization of the highly potent and selective covalent inhibitors targeting the lysine methyltransferases G9a/GLP

Z Feng, C Yang, Y Zhang, H Li, W Fang… - Journal of Medicinal …, 2023 - ACS Publications
Protein lysine methyltransferases G9a and GLP, which catalyze mono-and di-methylation of
histone H3K9 and nonhistone proteins, play important roles in diverse cellular processes …

H3K36 methyltransferases as cancer drug targets: rationale and perspectives for inhibitor development

DS Rogawski, J Grembecka… - Future Medicinal …, 2016 - Taylor & Francis
Methylation at histone 3, lysine 36 (H3K36) is a conserved epigenetic mark regulating gene
transcription, alternative splicing and DNA repair. Genes encoding H3K36 …