Targeting EHMT2/G9a for cancer therapy: Progress and perspective

S Jan, MI Dar, R Wani, J Sandey, I Mushtaq… - European Journal of …, 2021 - Elsevier
… h2 are essential histone methyltransferases for H3K9me3 on heterochromatin, and that
EHMT2 is a major H3K9me1 and H3K9me2 histone lysine methyltransferase of euchromatin and …

Targeting H3K9 methyltransferase G9a and its related molecule GLP as a potential therapeutic strategy for cancer

Z Rahman, MR Bazaz, G Devabattula… - … of Biochemical and …, 2021 - Wiley Online Library
histone methyltransferase G9a (KMT1C) and GLP or KMT1D are the members of family
Su(var)3-9, participate in mono- and di-methylation … The development of a potent inhibitor of G9a

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

Y Nishigaya, S Takase, T Sumiya… - Journal of Medicinal …, 2023 - ACS Publications
… (35) Moreover, discovery and development of G9a inhibitors has been a challenging task
in … (4 and 7 days) and western blotting analysis of histone methylation (7 and 12 days) in a …

The Role and Mechanism of the Histone Methyltransferase G9a in Tumors: Update

H Zhou, J Gui, L Zhu, Y Mi - OncoTargets and Therapy, 2024 - Taylor & Francis
… of G9a with many drugs is still under study. This article aims to summarize the role and
mechanism of G9a and its inhibitors in … progress in recent years to comprehensively understand …

Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with In Vivo …

O Rabal, E San Jose-Eneriz, X Agirre… - Journal of Medicinal …, 2021 - ACS Publications
… Despite recent progress in the development of non-nucleoside-… activity against G9a (EHMT2),
a histone methyltransferase … for the evaluation of in vivo efficacy of anticancer drugs. (43) …

Small molecules targeting selected histone methyltransferases (HMTs) for cancer treatment: current progress and novel strategies

D Li, X Peng, Z Hu, S Li, J Chen, W Pan - European journal of medicinal …, 2023 - Elsevier
… summarizes the recent progress in the development of histone methyltransferases (HMTs) …
SET-domain, along with the evaluation of the efficacy of G9a chemical inhibitors in various …

[HTML][HTML] Recent progress in DNA methyltransferase inhibitors as anticancer agents

Z Zhang, G Wang, Y Li, D Lei, J Xiang… - Frontiers in …, 2022 - frontiersin.org
… In order to promote the development of a DNA methyltransferase inhibitor as an anti-tumor
agent, … As an inhibitor of histone methyltransferase G9a, studies have shown that CM-272 can …

[HTML][HTML] Novel insights into histone lysine methyltransferases in cancer therapy: From epigenetic regulation to selective drugs

Q Liao, J Yang, S Ge, P Chai, J Fan, R Jia - Journal of Pharmaceutical …, 2023 - Elsevier
… to target KMTs involved in histone methylation and epigenetic regulation, but these … with
classical chemotherapeutic agents and small molecule-targeted drugs, EZH2 and G9a can …

[HTML][HTML] Advances in epigenetic cancer therapeutics

C Hillyar, KS Rallis, J Varghese - Cureus, 2020 - ncbi.nlm.nih.gov
… This review discusses recent advances in cancer epigenetics … Anticancer drugs that alter
IDH and TET enzyme activity have … histone lysine methyltransferase 2 (G9A), the histone-lysine …

[HTML][HTML] Novel G9a/DNMT first-in-class dual reversible inhibitor has potent antitumor effect in bladder cancer

WA Kwon, HK Seo - Translational Cancer Research, 2020 - ncbi.nlm.nih.gov
G9a (EHMT2), a histone methyltransferase that catalyzes … Recent studies (12,13) have
shown that the responses of type I interferon impact to the efficacy of chemotherapeutic agents. …