Histone-lysine N-methyltransferase EHMT2 (G9a) inhibition mitigates tumorigenicity in Myc-driven liver cancer.
Sign Up to like & getrecommendations! Published in 2023 at "Molecular oncology"
DOI: 10.1002/1878-0261.13417
Abstract: Hepatocellular carcinoma (HCC) is the third deadliest and sixth most common cancer in the world. Histone-lysine N-methyltransferase EHMT2 (also known as G9a) is a histone methyltransferase frequently overexpressed in many cancer types, including HCC. We… read more here.
Keywords: driven liver; histone; g9a; myc driven ... See more keywords
Structure‐Based Virtual Screening and in vitro and in vivo Analyses Revealed Potent Methyltransferase G9a Inhibitors as Prospective Anti‐Alzheimer's Agents
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200002
Abstract: G9a is a lysine methyltransferase able to di‐methylate lysine 9 of histone H3, promoting the repression of genes involved in learning and memory. Novel strategies based on synthesizing epigenetic drugs could regulate gene expression through… read more here.
Keywords: structure; virtual screening; g9a; based virtual ... See more keywords
Dual Targeting of G9a and DNA Methyltransferase‐1 for the Treatment of Experimental Cholangiocarcinoma
Sign Up to like & getrecommendations! Published in 2020 at "Hepatology"
DOI: 10.1002/hep.31642
Abstract: Cholangiocarcinoma (CCA) is a devastating disease often detected at advanced stages when surgery cannot be performed. Conventional and targeted systemic therapies perform poorly, and therefore effective drugs are urgently needed. Different epigenetic modifications occur in… read more here.
Keywords: dual targeting; methyltransferase; cholangiocarcinoma; dna methyltransferase ... See more keywords
Targeting EHMT2/ G9a for cancer therapy: progress and perspective.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2020.173827
Abstract: Euchromatic histone lysine methyltransferase-2, also known as G9a, is a ubiquitously expressed SET domain-containing histone lysine methyltransferase linked with both facultative and constitutive heterochromatin formation and transcriptional repression. It is an essential developmental gene and… read more here.
Keywords: targeting ehmt2; ehmt2 g9a; cancer therapy; cancer ... See more keywords
Discovery of Novel Substrate-Competitive Lysine Methyltransferase G9a Inhibitors as Anticancer Agents.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c02059
Abstract: Identification of structurally novel inhibitors of lysine methyltransferase G9a has been a subject of intense research in cancer epigenetics. Starting with the high-throughput screening (HTS) hit rac-10a obtained from the chemical library of the University… read more here.
Keywords: substrate competitive; methyltransferase g9a; discovery novel; g9a ... See more keywords
Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b02008
Abstract: 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 (GLP) have been reported. Herein, we report the identification of… read more here.
Keywords: crystal structure; glp; discovery; novel chemotype ... See more keywords
Human EHMT2/G9a activates p53 through methylation-independent mechanism
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DOI: 10.1038/onc.2016.258
Abstract: p53 is a critical tumor suppressor in humans. It functions mostly as a transcriptional factor and its activity is regulated by numerous post-translational modifications. Among different covalent modifications found on p53 the most controversial one… read more here.
Keywords: methylation; ehmt2 g9a; human ehmt2; hg9a ... See more keywords
G9a controls pluripotent-like identity and tumor-initiating function in human colorectal cancer
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DOI: 10.1038/s41388-020-01591-7
Abstract: Colorectal tumors are hierarchically organized and governed by populations of self-renewing cancer stem cells, representing one of the deadliest types of cancers worldwide. Emergence of cancer stemness phenotype depends on epigenetic reprogramming, associated with profound… read more here.
Keywords: cancer stem; colorectal cancer; cancer; g9a ... See more keywords
KDM4B histone demethylase and G9a regulate expression of vascular adhesion proteins in cerebral microvessels
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DOI: 10.1038/srep45005
Abstract: Intercellular adhesion molecule 1 (ICAM1) mediates the adhesion and transmigration of leukocytes across the endothelium, promoting inflammation. We investigated the epigenetic mechanism regulating ICAM1 expression. The pro-inflammatory cytokine TNF-α dramatically increased ICAM1 mRNA and protein… read more here.
Keywords: histone demethylase; kdm4b histone; adhesion; expression ... See more keywords
Low G9a expression is a tumor progression factor of colorectal cancer via IL-8 promotion.
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DOI: 10.1093/carcin/bgac050
Abstract: The histone methyltransferase G9a is expressed in various types of cancer cells, including colorectal cancer (CRC) cells. Interleukin (IL)-8, also known as C-X-C motif chemokine ligand 8 (CXCL8), is a chemokine that plays a pleiotropic… read more here.
Keywords: low g9a; expression; g9a; crc ... See more keywords
Cholesterol Biosynthesis Is Required for Cell Death in Response to G9A Inhibitor in Lung Cancer (P05-010-19).
Sign Up to like & getrecommendations! Published in 2019 at "Current developments in nutrition"
DOI: 10.1093/cdn/nzz030.p05-010-19
Abstract: Objectives G9A is a eukaryotic histone methyltransferase that contributes to transcriptional silencing of tumor suppressor genes by modulating histone 3 lysine 9 methylation (H3K9m). It has been recently suggested as a promising therapeutic target for… read more here.
Keywords: cell death; cholesterol biosynthesis; lung cancer; g9a ... See more keywords