A histone-lysine N-methyltransferase SETDB1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15047]
EC 2.1.1.366;
ERG-associated protein with SET domain;
ESET;
Histone H3-K9 methyltransferase 4;
H3-K9-HMTase 4;
Lysine N-methyltransferase 1E;
SET domain bifurcated 1
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 2 (100.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| s-adenosylhomocysteine | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
| 6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
This protein enables 9 target(s):
| Target | Category | Definition |
|---|---|---|
| DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
| chromatin binding | molecular function | Binding 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] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
| 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 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] |
| histone H3K9 monomethyltransferase activity | molecular function | Catalysis of the reaction: L-lysyl9-[histone H3] + S-adenosyl-L-methionine = H+ + N6-methyl-L-lysyl9-[histone H3] + S-adenosyl-L-homocysteine. This reaction is the addition of a methyl group to the unmethylated lysine residue at position 9 of histone H3, producing histone H3K9me. [RHEA:60288] |
| histone H3K9 trimethyltransferase activity | molecular function | Catalysis of the reaction: L-lysyl9-[histone H3] + 3 S-adenosyl-L-methionine = 3 H+ + N6,N6,N6-trimethyl-L-lysyl9-[histone H3] + 3 S-adenosyl-L-homocysteine. This reaction is the successive addition of three methyl groups to the unmethylated lysine residue at position 9 of histone H3, producing histone H3K9me3. [RHEA:60276] |
| promoter-specific chromatin binding | molecular function | Binding to a section of chromatin that is associated with gene promoter sequences of DNA. [PMID:19948729] |
This protein is located in 5 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] |
| chromosome | cellular component | A structure composed of a very long molecule of DNA and associated proteins (e.g. histones) that carries hereditary information. [ISBN:0198547684] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
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] |
This protein is involved in 6 target(s):
| Target | Category | Definition |
|---|---|---|
| chromatin remodeling | biological process | A dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820] |
| methylation | biological process | The process in which a methyl group is covalently attached to a molecule. [GOC:mah] |
| negative regulation of single stranded viral RNA replication via double stranded DNA intermediate | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of single stranded viral RNA replication via double stranded DNA intermediate. [GOC:go_curators] |
| positive regulation of DNA methylation-dependent heterochromatin formation | biological process | Any process that increases the rate, frequency, or extent of DNA methylation-dependent heterochromatin formation. [GOC:BHF] |
| negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| heterochromatin organization | biological process | Any process that results in the specification, formation or maintenance of the physical structure of eukaryotic heterochromatin, a compact and highly condensed form of chromatin. [GOC:mah] |