Proteins > Histone-lysine N-methyltransferase EHMT2
Page last updated: 2024-08-08 00:09:42
Histone-lysine N-methyltransferase EHMT2
A histone-lysine N-methyltransferase, H3 lysine-9 specific 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q96KQ7]
Synonyms
EC 2.1.1.-;
Euchromatic histone-lysine N-methyltransferase 2;
HLA-B-associated transcript 8;
Histone H3-K9 methyltransferase 3;
H3-K9-HMTase 3;
Lysine N-methyltransferase 1C;
Protein G9a
Research
Bioassay Publications (31)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 2 (6.45) | 29.6817 |
2010's | 26 (83.87) | 24.3611 |
2020's | 3 (9.68) | 2.80 |
Compounds (32)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bix 01294 | Homo sapiens (human) | Kd | 0.1300 | 1 | 1 |
unc 0638 | Homo sapiens (human) | Kd | 1.4200 | 1 | 1 |
brd4770 | Homo sapiens (human) | EC50 | 5.0000 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
unc 0638 | Homo sapiens (human) | K | 53.6000 | 1 | 1 |
Gliotoxin analogues from a marine-derived fungus, Penicillium sp., and their cytotoxic and histone methyltransferase inhibitory activities.Journal of natural products, , Jan-27, Volume: 75, Issue:1, 2012
Oncoepigenomics: making histone lysine methylation count.European journal of medicinal chemistry, , Volume: 56, 2012
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 26, Issue:18, 2016
SAH derived potent and selective EZH2 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
A medicinal chemistry perspective for targeting histone H3 lysine-79 methyltransferase DOT1L.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy.ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-MedChemComm, , May-01, Volume: 8, Issue:5, 2017
Discovery, design and synthesis of 6H-anthra[1,9-cd]isoxazol-6-one scaffold as G9a inhibitor through a combination of shape-based virtual screening and structure-based molecular modification.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
Selective inhibitors of protein methyltransferases.Journal of medicinal chemistry, , Feb-26, Volume: 58, Issue:4, 2015
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors†Electronic supplementary information (ESI) available. See DOI: 10.1039/c4md00274a.MedChemComm, , Dec-19, Volume: 5, Issue:12, 2014
Oncoepigenomics: making histone lysine methylation count.European journal of medicinal chemistry, , Volume: 56, 2012
Computer- and structure-based lead design for epigenetic targets.Bioorganic & medicinal chemistry, , Jun-15, Volume: 19, Issue:12, 2011
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.Journal of medicinal chemistry, , Dec-24, Volume: 52, Issue:24, 2009
Chemical probes for histone-modifying enzymes.Nature chemical biology, , Volume: 4, Issue:10, 2008
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
Recent progress in histone methyltransferase (G9a) inhibitors as anticancer agents.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.European journal of medicinal chemistry, , Dec-15, Volume: 184, 2019
Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Novel SAR for quinazoline inhibitors of EHMT1 and EHMT2.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 29, Issue:17, 2019
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Discovery, design and synthesis of 6H-anthra[1,9-cd]isoxazol-6-one scaffold as G9a inhibitor through a combination of shape-based virtual screening and structure-based molecular modification.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors†Electronic supplementary information (ESI) available. See DOI: 10.1039/c4md00274a.MedChemComm, , Dec-19, Volume: 5, Issue:12, 2014
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Oncoepigenomics: making histone lysine methylation count.European journal of medicinal chemistry, , Volume: 56, 2012
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells.Bioorganic chemistry, , Volume: 72, 2017
Discovery, design and synthesis of 6H-anthra[1,9-cd]isoxazol-6-one scaffold as G9a inhibitor through a combination of shape-based virtual screening and structure-based molecular modification.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
Enables
This protein enables 13 target(s):
Target | Category | Definition |
RNA polymerase II transcription regulatory region sequence-specific DNA binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls the transcription of a gene or cistron by RNA polymerase II. [GOC:txnOH] |
transcription corepressor binding | molecular function | Binding to a transcription corepressor, a protein involved in negative regulation of transcription via protein-protein interactions with transcription factors and other proteins that negatively regulate transcription. Transcription corepressors do not bind DNA directly, but rather mediate protein-protein interactions between repressing transcription factors and the basal transcription machinery. [GOC:krc] |
p53 binding | molecular function | Binding to one of the p53 family of proteins. [GOC:hjd] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
protein-lysine N-methyltransferase activity | molecular function | Catalysis of the transfer of a methyl group from S-adenosyl-L-methionine to the epsilon-amino group of a lysine residue in a protein substrate. [PMID:12054878] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
histone H3K9 methyltransferase activity | molecular function | Catalysis of the reaction: S-adenosyl-L-methionine + histone H3 L-lysine (position 9) = S-adenosyl-L-homocysteine + histone H3 N6-methyl-L-lysine (position 9). This reaction is the addition of up to three methyl groups to the lysine residue at position 9 of the histone H3 protein. [GOC:ai] |
histone H3K27 methyltransferase activity | molecular function | Catalysis of the reaction: S-adenosyl-L-methionine + histone H3 L-lysine (position 27) = S-adenosyl-L-homocysteine + histone H3 N6-methyl-L-lysine (position 27). This reaction is the addition of a methyl group to the lysine residue at position 27 of the histone H3 protein. [GOC:ai] |
C2H2 zinc finger domain binding | molecular function | Binding to a C2H2-type zinc finger domain of a protein. The C2H2 zinc finger is the classical zinc finger domain, in which two conserved cysteines and histidines co-ordinate a zinc ion. [GOC:BHF, GOC:mah, Pfam:PF00096] |
histone H3K56 methyltransferase activity | molecular function | Catalysis of the reaction: S-adenosyl-L-methionine + histone H3 L-lysine (position 56) = S-adenosyl-L-homocysteine + histone H3 N6-methyl-L-lysine (position 56). This reaction is the addition of a methyl group to the lysine residue at position 56 of the histone H3 protein. [PMID:23451023, PMID:28743002] |
histone H3K9me2 methyltransferase activity | molecular function | Catalysis of the reaction: N6,N6-dimethyl-L-lysyl9-[histone H3] + S-adenosyl-L-methionine = H+ + N6,N6,N6-trimethyl-L-lysyl9-[histone H3] + S-adenosyl-L-homocysteine. This reaction is the addition of a single methyl group to the dimethylated lysine residue at position 9 of histone H3, producing histone H3K9me3. [RHEA:60280] |
promoter-specific chromatin binding | molecular function | Binding to a section of chromatin that is associated with gene promoter sequences of DNA. [PMID:19948729] |
Located In
This protein is located in 3 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
nuclear speck | cellular component | A discrete extra-nucleolar subnuclear domain, 20-50 in number, in which splicing factors are seen to be localized by immunofluorescence microscopy. [http://www.cellnucleus.com/] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 20 target(s):
Target | Category | Definition |
regulation of DNA replication | biological process | Any process that modulates the frequency, rate or extent of DNA replication. [GOC:go_curators] |
DNA methylation-dependent heterochromatin formation | biological process | Repression of transcription by methylation of DNA, leading to the formation of heterochromatin. [GOC:mah] |
synaptonemal complex assembly | biological process | The cell cycle process in which the synaptonemal complex is formed. This is a structure that holds paired chromosomes together during prophase I of meiosis and that promotes genetic recombination. [ISBN:0198506732] |
spermatid development | biological process | The process whose specific outcome is the progression of a spermatid over time, from its formation to the mature structure. [GOC:dph, GOC:go_curators] |
long-term memory | biological process | The memory process that deals with the storage, retrieval and modification of information a long time (typically weeks, months or years) after receiving that information. This type of memory is typically dependent on gene transcription regulated by second messenger activation. [http://hebb.mit.edu/courses/9.03/lecture4.html, ISBN:0582227089] |
fertilization | biological process | The union of gametes of opposite sexes during the process of sexual reproduction to form a zygote. It involves the fusion of the gametic nuclei (karyogamy) and cytoplasm (plasmogamy). [GOC:tb, ISBN:0198506732] |
peptidyl-lysine dimethylation | biological process | The methylation of peptidyl-lysine to form peptidyl-N6,N6-dimethyl-L-lysine. [RESID:AA0075] |
regulation of protein modification process | biological process | Any process that modulates the frequency, rate or extent of the covalent alteration of one or more amino acid residues within a protein. [GOC:mah, GOC:tb] |
organ growth | biological process | The increase in size or mass of an organ. Organs are commonly observed as visibly distinct structures, but may also exist as loosely associated clusters of cells that function together as to perform a specific function. [GOC:bf, ISBN:0471245208, ISBN:0721662544] |
phenotypic switching | biological process | A reversible switch of a cell from one cell type or form to another, at a frequency above the expected frequency for somatic mutations. Phenotypic switching involves changes in cell morphology and altered gene expression patterns. For example, Candida albicans switches from white cells to opaque cells for sexual mating. Phenotypic switching also occurs in multicellular organisms; smooth muscle cells (SMCs) exhibit phenotypic transitions to allow rapid adaption to fluctuating environmental cues. [GOC:bf, GOC:di, PMID:12443899, PMID:22406749, PMID:8456504, Wikipedia:Phenotypic_switching] |
negative regulation of gene expression via chromosomal CpG island methylation | biological process | An epigenetic gene regulation mechanism that negatively regulates gene expression by methylation of cytosine residues in chromosomal CpG islands. CpG islands are genomic regions that contain a high frequency of the CG dinucleotide associated with the transcription start site of genes. [PMID:11898023, Wikipedia:Cpg_island] |
response to ethanol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ethanol stimulus. [GOC:go_curators] |
behavioral response to cocaine | biological process | Any process that results in a change in the behavior of an organism as a result of a cocaine stimulus. [GOC:jid] |
oocyte development | biological process | The process whose specific outcome is the progression of an oocyte over time, from initial commitment of the cell to its specific fate, to the fully functional differentiated cell. [GOC:go_curators] |
neuron fate specification | biological process | The process in which a cell becomes capable of differentiating autonomously into a neuron in an environment that is neutral with respect to the developmental pathway. Upon specification, the cell fate can be reversed. [GOC:dph] |
response to fungicide | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a fungicide stimulus. Fungicides are chemicals used to kill fungi. [GOC:dph] |
cellular response to cocaine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:mah] |
cellular response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organism exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:krc, GOC:mah] |
negative regulation of autophagosome assembly | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of autophagosome assembly. [GO_REF:0000058, GOC:als, GOC:autophagy, GOC:TermGenie, PMID:21975012] |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |