A lysine-specific demethylase 4C that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H3R0]
EC 1.14.11.66;
Gene amplified in squamous cell carcinoma 1 protein;
GASC-1 protein;
JmjC domain-containing histone demethylation protein 3C;
Jumonji domain-containing protein 2C;
[histone H3]-trimethyl-L-lysine(9) demethylase 4C
| 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 | 10 (76.92) | 24.3611 |
| 2020's | 3 (23.08) | 2.80 |
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| pyrazole | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| pyrazole | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
| nitrazepam | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| nitrazepam | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
| 2,4-pyridinedicarboxylic acid | Homo sapiens (human) | IC50 | 7.1710 | 12 | 19 |
| 2,4-pyridinedicarboxylic acid | Homo sapiens (human) | Ki | 6.5011 | 2 | 2 |
| daminozide | Homo sapiens (human) | IC50 | 2,500.0000 | 1 | 1 |
| toxoflavin | Homo sapiens (human) | IC50 | 0.5205 | 2 | 2 |
| n-acetylglutamic acid | Homo sapiens (human) | IC50 | 2,070.0000 | 1 | 1 |
| d-2-hydroxyglutarate | Homo sapiens (human) | IC50 | 79.0000 | 1 | 1 |
| alpha-hydroxyglutarate, (l)-isomer | Homo sapiens (human) | IC50 | 97.0000 | 1 | 1 |
| 5-carboxy-8-hydroxyquinoline | Homo sapiens (human) | IC50 | 0.4770 | 3 | 3 |
| (1R,2S)-tranylcypromine hydrochloride | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| N-[2-furanyl-(8-hydroxy-7-quinolinyl)methyl]-2-methylpropanamide | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| oxalylglycine | Homo sapiens (human) | IC50 | 141.0438 | 5 | 13 |
| geldanamycin | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| tanespimycin | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| 3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid | Homo sapiens (human) | IC50 | 16.4762 | 2 | 8 |
This protein enables 9 target(s):
| Target | Category | Definition |
|---|---|---|
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| nuclear receptor coactivator activity | molecular function | A transcription coactivator activity that activates or increases the transcription of specific gene sets via binding to a DNA-bound nuclear receptor, either on its own or as part of a complex. Coactivators often act by altering chromatin structure and modifications. For example, one class of transcription coregulators 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. A fourth class of coactivator activity is the bridging of a DNA-binding transcription factor to the general (basal) transcription machinery. The Mediator complex, which bridges sequence-specific DNA binding transcription factors and RNA polymerase, is also a transcription coactivator. [GOC:dph, GOC:tb] |
| histone demethylase activity | molecular function | Catalysis of the removal of a methyl group from a histone. [GOC:mah] |
| histone H3K9 demethylase activity | molecular function | Catalysis of the removal of a methyl group from a modified lysine residue at position 9 of the histone H3 protein. [PMID:16362057] |
| nuclear androgen receptor binding | molecular function | Binding to a nuclear androgen receptor. [GOC:ai] |
| histone H3K36 demethylase activity | molecular function | Catalysis of the removal of a methyl group from a modified lysine residue at position 36 of the histone H3 protein. This is a dioxygenase reaction that is dependent on Fe(II) and 2-oxoglutarate. [PMID:16362057] |
| H3K9me3 modified histone binding | molecular function | Binding to a histone H3 in which the lysine residue at position 9 has been modified by trimethylation. [PMID:30110338] |
| histone H3K9me2/H3K9me3 demethylase activity | molecular function | Catalysis of the removal of a methyl group from a tri or a dimethyl-lysine residue at position 9 of the histone H3 protein. This is a dioxygenase reaction that is dependent on Fe(II) and 2-oxoglutarate. [PMID:20208542, PMID:20531378] |
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|---|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
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 part of 2 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] |
| pericentric heterochromatin | cellular component | Heterochromatin 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] |
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|---|---|
| blastocyst formation | biological process | The initial formation of a blastocyst from a solid ball of cells known as a morula. [GOC:dph, ISBN:0124020607, ISBN:0198542771] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| stem cell population maintenance | biological process | The process by which an organism or tissue maintains a population of stem cells of a single type. This can be achieved by a number of mechanisms: stem cell asymmetric division maintains stem cell numbers; stem cell symmetric division increases them; maintenance of a stem cell niche maintains the conditions for commitment to the stem cell fate for some types of stem cell; stem cells may arise de novo from other cell types. [GOC:mah, ISBN:0878932437] |
| androgen receptor signaling pathway | biological process | The series of molecular signals initiated by androgen binding to its receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| regulation of androgen receptor signaling pathway | biological process | Any process that modulates the rate, frequency, or extent of the androgen receptor signaling pathway. [GOC:dph] |
| regulation of stem cell differentiation | biological process | Any process that modulates the frequency, rate or extent of stem cell differentiation. [GOC:obol] |
| regulation of gene expression | biological process | Any process that modulates 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] |
| 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] |