Page last updated: 2024-08-07 23:52:14

Histone-lysine N-methyltransferase EZH2

A histone-lysine N-methyltransferase EZH2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15910]

Synonyms

EC 2.1.1.356;
ENX-1;
Enhancer of zeste homolog 2;
Lysine N-methyltransferase 6

Research

Bioassay Publications (20)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (40.00)24.3611
2020's12 (60.00)2.80

Compounds (10)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
3-deazaneplanocinHomo sapiens (human)IC500.080011
tanshinoneHomo sapiens (human)IC508.900011
przewaquinone dHomo sapiens (human)IC500.550022
przewaquinone dHomo sapiens (human)Ki0.194022
tanshinone ii aHomo sapiens (human)IC5028.100011
s-adenosylhomocysteineHomo sapiens (human)IC5024.840055
epz005687Homo sapiens (human)IC508.170977
epz005687Homo sapiens (human)Ki0.024022
epz-6438Homo sapiens (human)IC500.03271414
epz-6438Homo sapiens (human)Ki0.002511
gsk-2816126Homo sapiens (human)IC500.03501010
gsk-2816126Homo sapiens (human)Ki0.000588
gsk343Homo sapiens (human)IC501.025564
gsk343Homo sapiens (human)Ki0.001211
1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamideHomo sapiens (human)IC500.017855

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
epz005687Homo sapiens (human)EC502.900011
epz-6438Homo sapiens (human)EC500.060499
1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamideHomo sapiens (human)EC500.080011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
gsk343Homo sapiens (human)Ki,app0.001210

Enables

This protein enables 16 target(s):

TargetCategoryDefinition
RNA polymerase II cis-regulatory region sequence-specific DNA bindingmolecular functionBinding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018]
RNA polymerase II core promoter sequence-specific DNA bindingmolecular functionBinding to a DNA sequence that is part of the core promoter of a RNA polymerase II-transcribed gene. [GOC:pg, GOC:txnOH, PMID:12381658]
transcription corepressor bindingmolecular functionBinding 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]
chromatin bindingmolecular functionBinding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130]
transcription corepressor activitymolecular functionA transcription coregulator activity that represses or decreases the transcription of specific gene sets via binding to a DNA-bound DNA-binding transcription factor, either on its own or as part of a complex. Corepressors often act by altering chromatin structure and modifications. For example, one class of transcription corepressors modifies chromatin structure through covalent modification of histones. A second class remodels the conformation of chromatin in an ATP-dependent fashion. A third class modulates interactions of DNA-bound DNA-binding transcription factors with other transcription coregulators. [GOC:txnOH-2018, PMID:10213677, PMID:16858867]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
protein-lysine N-methyltransferase activitymolecular functionCatalysis 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]
chromatin DNA bindingmolecular functionBinding to DNA that is assembled into chromatin. [GOC:mah]
histone methyltransferase activitymolecular functionCatalysis of the reaction: S-adenosyl-L-methionine + histone = S-adenosyl-L-homocysteine + methyl-histone. Histone methylation generally occurs on either an arginine or a lysine residue. [GOC:curators]
ribonucleoprotein complex bindingmolecular functionBinding to a complex of RNA and protein. [GOC:bf, GOC:go_curators, GOC:vk]
histone H3K27 methyltransferase activitymolecular functionCatalysis 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]
primary miRNA bindingmolecular functionBinding to a primary microRNA (pri-miRNA) transcript, an RNA molecule that is processed into a short hairpin-shaped structure called a pre-miRNA and finally into a functional miRNA. Both double-stranded and single-stranded regions of a pri-miRNA are required for binding. [GOC:sl, PMID:15531877, PMID:15574589]
lncRNA bindingmolecular functionBinding to a long noncoding RNA (lncRNA). [PMID:25578728]
histone H3 methyltransferase activitymolecular functionCatalysis of the reaction: S-adenosyl-L-methionine + a histone H3 = S-adenosyl-L-homocysteine + a methylated histone H3. Histone methylation generally occurs on either an arginine or a lysine residue. [PMID:28450737]
histone H3K27 trimethyltransferase activitymolecular functionCatalysis of the reaction: L-lysyl27-[histone H3] + 3 S-adenosyl-L-methionine = 3 H+ + N6,N6,N6-trimethyl-L-lysyl27-[histone H3] + 3 S-adenosyl-L-homocysteine. This reaction is the successive addition of three methyl groups to the unmethylated lysine residue at position 27 of histone H3, producing histone H3K27me3. [RHEA:60292]
promoter-specific chromatin bindingmolecular functionBinding to a section of chromatin that is associated with gene promoter sequences of DNA. [PMID:19948729]

Located In

This protein is located in 5 target(s):

TargetCategoryDefinition
chromosome, telomeric regioncellular componentThe end of a linear chromosome, required for the integrity and maintenance of the end. A chromosome telomere usually includes a region of telomerase-encoded repeats the length of which rarely exceeds 20 bp each and that permits the formation of a telomeric loop (T-loop). The telomeric repeat region is usually preceded by a sub-telomeric region that is gene-poor but rich in repetitive elements. Some telomeres only consist of the latter part (for eg. D. melanogaster telomeres). [GOC:elh]
nucleuscellular componentA 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]
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
pronucleuscellular componentThe nucleus of either the ovum or the spermatozoon following fertilization. Thus, in the fertilized ovum, there are two pronuclei, one originating from the ovum, the other from the spermatozoon that brought about fertilization; they approach each other, but do not fuse until just before the first cleavage, when each pronucleus loses its membrane to release its contents. [ISBN:0198506732]
synapsecellular componentThe junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110]

Active In

This protein is active in 2 target(s):

TargetCategoryDefinition
chromosomecellular componentA structure composed of a very long molecule of DNA and associated proteins (e.g. histones) that carries hereditary information. [ISBN:0198547684]
nucleuscellular componentA 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 4 target(s):

TargetCategoryDefinition
chromatincellular componentThe ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130]
chromatin silencing complexcellular componentAny protein complex that mediates changes in chromatin structure that result in transcriptional silencing. [GOC:mah]
pericentric heterochromatincellular componentHeterochromatin that is located adjacent to the CENP-A rich centromere 'central core' and characterized by methylated H3 histone at lysine 9 (H3K9me2/H3K9me3). [PMID:12019236, PMID:20206496, PMID:21437270, PMID:22729156, PMID:9413993]
ESC/E(Z) complexcellular componentA multimeric protein complex that can methylate lysine-27 and lysine-9 residues of histone H3. In Drosophila the core subunits of the complex include ESC, E(Z), CAF1 (NURF-55) and SU(Z)12. In mammals the core subunits of the complex include EED, EZH2, SUZ12 and RBBP4. [GOC:bf, GOC:sp, PMID:12408863, PMID:12408864, PMID:20064375]

Involved In

This protein is involved in 47 target(s):

TargetCategoryDefinition
G1/S transition of mitotic cell cyclebiological processThe mitotic cell cycle transition by which a cell in G1 commits to S phase. The process begins with the build up of G1 cyclin-dependent kinase (G1 CDK), resulting in the activation of transcription of G1 cyclins. The process ends with the positive feedback of the G1 cyclins on the G1 CDK which commits the cell to S phase, in which DNA replication is initiated. [GOC:mtg_cell_cycle]
negative regulation of transcription by RNA polymerase IIbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH]
chromatin organizationbiological processThe assembly or remodeling of chromatin composed of DNA complexed with histones, other associated proteins, and sometimes RNA. [PMID:20404130]
regulation of DNA-templated transcriptionbiological processAny process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
positive regulation of cell population proliferationbiological processAny process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators]
positive regulation of epithelial to mesenchymal transitionbiological processAny process that increases the rate, frequency, or extent of epithelial to mesenchymal transition. Epithelial to mesenchymal transition is where an epithelial cell loses apical/basolateral polarity, severs intercellular adhesive junctions, degrades basement membrane components and becomes a migratory mesenchymal cell. [GOC:BHF, GOC:dph, GOC:tb]
regulation of gliogenesisbiological processAny process that modulates the frequency, rate or extent of gliogenesis, the formation of mature glia. [GOC:ef]
skeletal muscle satellite cell maintenance involved in skeletal muscle regenerationbiological processAny process by which the number of skeletal muscle satellite cells in a skeletal muscle is maintained during muscle regeneration. There are at least three mechanisms by which this is achieved. Skeletal muscle satellite stem cell asymmetric division ensures satellite stem cell numbers are kept constant. Symmetric division of these cells amplifies the number of skeletal muscle satellite stem cells. Some adult skeletal muscle myoblasts (descendants of activated satellite cells) can develop back into quiescent satellite cells, replenishing the overall pool of satellite cells. [GOC:dph, GOC:ef, GOC:mtg_muscle, GOC:tb, PMID:23303905]
cardiac muscle hypertrophy in response to stressbiological processThe physiological enlargement or overgrowth of all or part of the heart muscle due to an increase in size (not length) of individual cardiac muscle fibers, without cell division, as a result of a disturbance in organismal or cellular homeostasis. [GOC:BHF, GOC:mtg_cardiac_conduct_nov11, GOC:mtg_muscle]
cerebellar cortex developmentbiological processThe process whose specific outcome is the progression of the cerebellar cortex over time, from its formation to the mature structure. The cerebellar cortex is a thin mantle of gray matter that covers the surface of each cerebral hemisphere. It has a characteristic morphology with convolutions (gyri) and crevices (sulci) that have specific functions. Six layers of nerve cells and the nerve pathways that connect them comprise the cerebellar cortex. Together, these regions are responsible for the processes of conscious thought, perception, emotion and memory as well as advanced motor function. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0838580343]
hippocampus developmentbiological processThe progression of the hippocampus over time from its initial formation until its mature state. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0878937420, UBERON:0002421]
B cell differentiationbiological processThe process in which a precursor cell type acquires the specialized features of a B cell. A B cell is a lymphocyte of B lineage with the phenotype CD19-positive and capable of B cell mediated immunity. [GO_REF:0000022, GOC:mah]
keratinocyte differentiationbiological processThe process in which a relatively unspecialized cell acquires specialized features of a keratinocyte. [GOC:dph, GOC:mah, GOC:sdb_2009, GOC:tb]
positive regulation of cell migrationbiological processAny process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators]
regulatory ncRNA-mediated heterochromatin formationbiological processA heterochromatin formation-based gene silencing process mediated by a regulatory non-coding RNA molecule that occur before the beginnning of trancription. [PMID:19239886, PMID:21420348]
subtelomeric heterochromatin formationbiological processThe compaction of chromatin into heterochromatin at the subtelomeric region. [GOC:mah, PMID:10219245, PMID:26205977]
methylationbiological processThe process in which a methyl group is covalently attached to a molecule. [GOC:mah]
response to estradiolbiological processAny 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 stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123]
negative regulation of transcription elongation by RNA polymerase IIbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of transcription elongation, the extension of an RNA molecule after transcription initiation and promoter clearance by the addition of ribonucleotides, catalyzed by RNA polymerase II. [GOC:mah, GOC:txnOH]
cellular response to trichostatin Abiological processAny 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 trichostatin A stimulus. [GOC:yaf, PMID:20181743]
protein modification processbiological processThe covalent alteration of one or more amino acids occurring in proteins, peptides and nascent polypeptides (co-translational, post-translational modifications). Includes the modification of charged tRNAs that are destined to occur in a protein (pre-translation modification). [GOC:bf, GOC:jl]
hepatocyte homeostasisbiological processAny biological process involved in the maintenance of the steady-state number of hepatocytes within a population of cells. Hepatocytes are specialized epithelial cells of the liver that are organized into interconnected plates called lobules. [CL:0000182, GOC:nhn, PMID:19878874]
regulation of circadian rhythmbiological processAny process that modulates the frequency, rate or extent of a circadian rhythm. A circadian rhythm is a biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:dph, GOC:jl, GOC:tb]
positive regulation of MAP kinase activitybiological processAny process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators]
positive regulation of GTPase activitybiological processAny process that activates or increases the activity of a GTPase. [GOC:jl, GOC:mah]
negative regulation of keratinocyte differentiationbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of keratinocyte differentiation. [GOC:go_curators]
negative regulation of gene expression, epigeneticbiological processAn epigenetic process that silences gene expression at specific genomic regions through chromatin remodeling either by modifying higher order chromatin fiber structure, nucleosomal histones, or the cytosine DNA methylation. [PMID:22243696]
negative regulation of DNA-templated transcriptionbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
negative regulation of retinoic acid receptor signaling pathwaybiological processAny process that stops, prevents, or reduces the frequency, rate or extent of retinoic acid receptor signaling pathway activity. [GOC:dgh]
rhythmic processbiological processAny process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid]
stem cell differentiationbiological processThe process in which a relatively unspecialized cell acquires specialized features of a stem cell. A stem cell is a cell that retains the ability to divide and proliferate throughout life to provide progenitor cells that can differentiate into specialized cells. [CL:0000034, GOC:isa_complete]
negative regulation of striated muscle cell differentiationbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of striated muscle cell differentiation. [CL:0000737, GOC:ai]
synaptic transmission, GABAergicbiological processThe vesicular release of gamma-aminobutyric acid (GABA). from a presynapse, across a chemical synapse, the subsequent activation of GABA receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, ISBN:0126603030]
cellular response to hydrogen peroxidebiological processAny 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 hydrogen peroxide (H2O2) stimulus. [CHEBI:16240, GOC:mah]
G1 to G0 transitionbiological processA cell cycle arrest process that results in arrest during G1 phase, whereupon the cell enters a specialized resting state known as G0 or quiescence. [GOC:mah, GOC:mtg_cell_cycle, ISBN:0815316194]
protein localization to chromatinbiological processAny process in which a protein is transported to, or maintained at, a part of a chromosome that is organized into chromatin. [GOC:mah]
positive regulation of protein serine/threonine kinase activitybiological processAny process that increases the rate, frequency, or extent of protein serine/threonine kinase activity. [GOC:mah]
regulation of kidney developmentbiological processAny process that modulates the rate, frequency or extent of kidney development. Kidney development is the process whose specific outcome is the progression of the kidney over time, from its formation to the mature structure. The kidney is an organ that filters the blood and excretes the end products of body metabolism in the form of urine. [GOC:dph, GOC:tb, GOC:yaf]
liver regenerationbiological processThe regrowth of lost or destroyed liver. [GOC:gap, PMID:19447520]
facultative heterochromatin formationbiological processThe compaction of chromatin into a conformation that is refactory to transcription but that be converted to euchromatin and allow transcription in specific contexts. These can be temporal (e.g., developmental states or specific cell-cycle stages), spatial (e.g., nuclear localization changes from the center to the periphery or vice versa due to exogenous factors/signals), or parental/heritable (e.g., monoallelic gene expression). [PMID:17936700]
positive regulation of dendrite developmentbiological processAny process that activates or increases the frequency, rate or extent of dendrite development. [GOC:TermGenie]
negative regulation of cytokine production involved in inflammatory responsebiological processAny process that stops, prevents or reduces the frequency, rate or extent of cytokine production involved in inflammatory response. [GOC:TermGenie]
positive regulation of cell cycle G1/S phase transitionbiological processAny signaling pathway that activates or increases the activity of a cell cycle cyclin-dependent protein kinase to modulate the switch from G1 phase to S phase of the cell cycle. [GO_REF:0000058, GOC:mtg_cell_cycle, GOC:TermGenie]
response to tetrachloromethanebiological processAny 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 tetrachloromethane stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:7852267]
negative regulation of G1/S transition of mitotic cell cyclebiological processAny signaling pathway that decreases or inhibits the activity of a cell cycle cyclin-dependent protein kinase to modulate the switch from G1 phase to S phase of the mitotic cell cycle. [GOC:mtg_cell_cycle]
negative regulation of stem cell differentiationbiological processAny process that stops, prevents or reduces the frequency, rate or extent of stem cell differentiation. [GOC:obol]
heterochromatin formationbiological processAn epigenetic gene silencing mechanism in which chromatin is compacted into heterochromatin, resulting in a chromatin conformation refractory to transcription. This process starts with heterochromatin nucleation, its spreading, and ends with heterochromatin boundary formation. [PMID:25192661, PMID:33827924]