Proteins > Lysine-specific demethylase 4E
Page last updated: 2024-08-07 20:59:41
Lysine-specific demethylase 4E
A lysine-specific demethylase 4E that is encoded in the genome of human. [PRO:DNx, UniProtKB:B2RXH2]
Synonyms
EC 1.14.11.66;
KDM4D-like protein;
Lysine-specific demethylase 4D-like;
[histone H3]-trimethyl-L-lysine(9) demethylase 4E
Research
Bioassay Publications (10)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (10.00) | 29.6817 |
| 2010's | 6 (60.00) | 24.3611 |
| 2020's | 3 (30.00) | 2.80 |
Compounds (22)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| butyric acid | Homo sapiens (human) | IC50 | 10,000.0000 | 1 | 1 |
| quinolinic acid | Homo sapiens (human) | IC50 | 5,000.0000 | 1 | 1 |
| succinic acid | Homo sapiens (human) | IC50 | 710.0000 | 1 | 1 |
| fenoldopam | Homo sapiens (human) | Ki | 1.9200 | 1 | 1 |
| beta-lapachone | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| beta-lapachone | Homo sapiens (human) | Ki | 3.5500 | 1 | 1 |
| vorinostat | Homo sapiens (human) | IC50 | 277.0000 | 4 | 4 |
| succinylacetone | Homo sapiens (human) | IC50 | 23.9000 | 1 | 1 |
| 2,5-pyridinedicarboxylic acid | Homo sapiens (human) | IC50 | 180.0000 | 1 | 1 |
| 3,4-pyridinedicarboxylic acid | Homo sapiens (human) | IC50 | 10,000.0000 | 1 | 1 |
| 2,4-pyridinedicarboxylic acid | Homo sapiens (human) | IC50 | 3.8548 | 2 | 2 |
| 2,4-pyridinedicarboxylic acid | Homo sapiens (human) | Ki | 914.0000 | 1 | 1 |
| 3,5-pyridinedicarboxylic acid | Homo sapiens (human) | IC50 | 10,000.0000 | 1 | 1 |
| dipicolinic acid | Homo sapiens (human) | IC50 | 120.0000 | 1 | 1 |
| daminozide | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| carbidopa | Homo sapiens (human) | Ki | 1.9800 | 1 | 1 |
| trichostatin a | Homo sapiens (human) | IC50 | 28.4000 | 1 | 1 |
| fumaric acid | Homo sapiens (human) | IC50 | 1,600.0000 | 1 | 1 |
| 5-carboxy-8-hydroxyquinoline | Homo sapiens (human) | IC50 | 0.8027 | 6 | 6 |
| (1R,2S)-tranylcypromine hydrochloride | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| oxalylglycine | Homo sapiens (human) | IC50 | 89.0000 | 2 | 2 |
| baicalein | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| baicalein | Homo sapiens (human) | Ki | 4.3300 | 1 | 1 |
| myricetin | Homo sapiens (human) | IC50 | 3.0000 | 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 | 19.9526 | 1 | 1 |
Drugs with Other Measurements
Recent Advances with KDM4 Inhibitors and Potential Applications.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
Inhibitors of histone demethylases.Bioorganic & medicinal chemistry, , Jun-15, Volume: 19, Issue:12, 2011
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer.Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.MedChemComm, , Dec-01, Volume: 5, Issue:12, 2014
Inhibitors of histone demethylases.Bioorganic & medicinal chemistry, , Jun-15, Volume: 19, Issue:12, 2011
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Structure-Based Design of Selective Fat Mass and Obesity Associated Protein (FTO) Inhibitors.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Recent Progress in Histone Demethylase Inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.MedChemComm, , Dec-01, Volume: 5, Issue:12, 2014
Oncoepigenomics: making histone lysine methylation count.European journal of medicinal chemistry, , Volume: 56, 2012
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.MedChemComm, , Dec-01, Volume: 5, Issue:12, 2014
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| 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] |
| 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] |
Located In
This protein is located in 2 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] |
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 2 target(s):
| Target | Category | Definition |
|---|
| 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] |