Proteins > Lysine-specific demethylase 4A
Page last updated: 2024-08-07 23:05:15
Lysine-specific demethylase 4A
A lysine-specific demethylase 4A that is encoded in the genome of human. [PRO:DNx, UniProtKB:O75164]
Synonyms
EC 1.14.11.66;
EC 1.14.11.69;
JmjC domain-containing histone demethylation protein 3A;
Jumonji domain-containing protein 2A;
[histone H3]-trimethyl-L-lysine(36) demethylase 4A;
[histone H3]-trimethyl-L-lysine(9) demethylase 4A
Research
Bioassay Publications (13)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (7.69) | 29.6817 |
| 2010's | 8 (61.54) | 24.3611 |
| 2020's | 4 (30.77) | 2.80 |
Compounds (12)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Recent Advances with KDM4 Inhibitors and Potential Applications.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
Rational design, synthesis and biological profiling of new KDM4C inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Recent Advances with KDM4 Inhibitors and Potential Applications.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
Recent Progress in Histone Demethylase Inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 59, Issue:4, 2016
Recent Advances with KDM4 Inhibitors and Potential Applications.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
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
Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: introduction of an additional carboxyl group at the C-2 position of quinoline.European journal of medicinal chemistry, , Nov-13, Volume: 105, 2015
Oncoepigenomics: making histone lysine methylation count.European journal of medicinal chemistry, , Volume: 56, 2012
Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 29, Issue:10, 2019
Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Lysine demethylases inhibitors.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Enables
This protein enables 9 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| histone demethylase activity | molecular function | Catalysis of the removal of a methyl group from a histone. [GOC:mah] |
| methylated histone binding | molecular function | Binding to a histone in which a residue has been modified by methylation. [GOC:bf, PMID:14585615] |
| 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] |
| histone H3K36me2/H3K36me3 demethylase activity | molecular function | Catalysis of the removal of a methyl group from a tri- or a dimethyl-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:21914792] |
| 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 4 target(s):
| Target | Category | Definition |
|---|
| fibrillar center | cellular component | A structure found most metazoan nucleoli, but not usually found in lower eukaryotes; surrounded by the dense fibrillar component; the zone of transcription from multiple copies of the pre-rRNA genes is in the border region between these two structures. [PMID:10754561] |
| 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] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
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 2 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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 11 target(s):
| Target | Category | Definition |
|---|
| negative regulation of autophagy | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| positive regulation of gene expression | biological process | Any process that increases 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] |
| 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] |
| cardiac muscle hypertrophy in response to stress | biological process | The 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] |
| apoptotic chromosome condensation | biological process | The compaction of chromatin during apoptosis. [GOC:mah] |
| response to nutrient levels | 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 stimulus reflecting the presence, absence, or concentration of nutrients. [GOC:mah] |
| positive regulation of neuron differentiation | biological process | Any process that activates or increases the frequency, rate or extent of neuron differentiation. [GOC:go_curators] |
| negative regulation of DNA-templated transcription | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| negative regulation of astrocyte differentiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of astrocyte differentiation. [GOC:vp, PMID:15139015] |
| 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] |
| 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] |