Lysine-specific histone demethylase 1A

A lysine-specific histone demethylase 1A that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60341]

Synonyms

EC 1.14.99.66;
BRAF35-HDAC complex protein BHC110;
Flavin-containing amine oxidase domain-containing protein 2;
[histone H3]-dimethyl-L-lysine(4) FAD-dependent demethylase 1A

Research

Bioassay Publications (46)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	1 (2.17)	29.6817
2010's	30 (65.22)	24.3611
2020's	15 (32.61)	2.80

Compounds (48)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
berberine	Homo sapiens (human)	IC50	6.9700	1	1
phenelzine	Homo sapiens (human)	Ki	11.7000	4	4
raloxifene	Homo sapiens (human)	IC50	2.0800	1	1
vorinostat	Homo sapiens (human)	IC50	100.0000	2	2
2-phenylcyclopropan-1-amine	Homo sapiens (human)	IC50	65.1025	4	4
hesperidin	Homo sapiens (human)	IC50	19.1600	1	1
palmatine	Homo sapiens (human)	IC50	12.2300	1	1
tranylcypromine	Homo sapiens (human)	IC50	31.7023	13	13
tranylcypromine	Homo sapiens (human)	Ki	208.2200	5	5
(1S,2R)-tranylcypromine	Homo sapiens (human)	IC50	16.4700	7	7
(1S,2R)-tranylcypromine	Homo sapiens (human)	Ki	159.5333	2	3
dehydrocorydalin	Homo sapiens (human)	IC50	2.4400	1	1
baicalin	Homo sapiens (human)	IC50	3.1900	3	3
hesperetin	Homo sapiens (human)	IC50	78.7600	1	1
columbamine	Homo sapiens (human)	IC50	0.4700	2	2
jatrorrhizine	Homo sapiens (human)	IC50	1.5500	1	1
higenamine	Homo sapiens (human)	IC50	1.4700	1	1
tanshinone	Homo sapiens (human)	IC50	16.4500	2	2
cryptotanshinone	Homo sapiens (human)	IC50	9.0200	1	1
epiberberine	Homo sapiens (human)	IC50	0.1400	4	4
erlotinib	Homo sapiens (human)	IC50	35.8000	1	1
resveratrol	Homo sapiens (human)	IC50	12.6000	2	2
curcumin	Homo sapiens (human)	IC50	9.6000	1	1
capsaicin	Homo sapiens (human)	IC50	0.6000	3	3
(1R,2S)-tranylcypromine hydrochloride	Homo sapiens (human)	IC50	14.9500	2	2
N5-(2-chloro-6-phenoxybenzyl)-1H-1,2,4-triazole-3,5-diamine	Homo sapiens (human)	IC50	1.1700	4	4
N5-(2-chloro-6-phenoxybenzyl)-1H-1,2,4-triazole-3,5-diamine	Homo sapiens (human)	Ki	2.2000	1	1
mdl 72527	Homo sapiens (human)	IC50	100.0000	1	1
wogonoside	Homo sapiens (human)	IC50	2.9800	1	1
quercetin	Homo sapiens (human)	IC50	1.2600	1	1
biochanin a	Homo sapiens (human)	IC50	2.9500	3	3
quercetin 3-o-glucopyranoside	Homo sapiens (human)	IC50	0.9500	1	1
quercetin 3-o-glucopyranoside	Homo sapiens (human)	Ki	1.0000	1	1
rutin	Homo sapiens (human)	IC50	2.1600	1	1
baicalein	Homo sapiens (human)	IC50	12.5000	1	1
diosmetin	Homo sapiens (human)	IC50	27.9000	1	1
diosmin	Homo sapiens (human)	IC50	10.1400	1	1
mangostin	Homo sapiens (human)	IC50	2.8100	1	1
wogonin	Homo sapiens (human)	IC50	8.8700	1	1
rosmarinic acid	Homo sapiens (human)	IC50	20.9300	2	2
afimoxifene	Homo sapiens (human)	IC50	50.0000	1	1
icaritin	Homo sapiens (human)	IC50	64.4900	1	1
icariin	Homo sapiens (human)	IC50	26.4400	1	1
baohuoside i	Homo sapiens (human)	IC50	16.7000	1	1
salvianolic acid B	Homo sapiens (human)	IC50	0.1100	2	2
Diosmetin 7-O-beta-D-glucopyranoside	Homo sapiens (human)	IC50	21.8300	1	1
Dihydrotanshinone I	Homo sapiens (human)	IC50	15.8500	2	2
N-(3-ethynylphenyl)-6,7-dimethoxy-4-quinazolinamine	Homo sapiens (human)	IC50	50.0000	1	1
1-(4-methyl-1-piperazinyl)-2-[[(1R,2S)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]ethanone	Homo sapiens (human)	IC50	0.0258	4	4
gsk2879552	Homo sapiens (human)	IC50	50.6981	8	8
gsk2879552	Homo sapiens (human)	Ki	1.1365	3	3
osimertinib	Homo sapiens (human)	IC50	3.9800	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
(1R,2S)-tranylcypromine hydrochloride	Homo sapiens (human)	Kd	46.3000	1	1
polymyxin b(1)	Homo sapiens (human)	Kd	0.4630	1	1
gsk2879552	Homo sapiens (human)	EC50	0.0540	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
tranylcypromine	Homo sapiens (human)	Kinact	477.0000	1	1
N5-(2-chloro-6-phenoxybenzyl)-1H-1,2,4-triazole-3,5-diamine	Homo sapiens (human)	Ka	0.0489	1	1

Enables

This protein enables 21 target(s):

Target	Category	Definition
p53 binding	molecular function	Binding to one of the p53 family of proteins. [GOC:hjd]
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]
transcription coactivator activity	molecular function	A transcription coregulator activity that activates or increases 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. Coactivators often act by altering chromatin structure and modifications. For example, one class of transcription coactivators 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:txnOH-2018, PMID:10213677, PMID:16858867]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
oxidoreductase activity	molecular function	Catalysis of an oxidation-reduction (redox) reaction, a reversible chemical reaction in which the oxidation state of an atom or atoms within a molecule is altered. One substrate acts as a hydrogen or electron donor and becomes oxidized, while the other acts as hydrogen or electron acceptor and becomes reduced. [GOC:go_curators]
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]
demethylase activity	molecular function	Catalysis of the removal of a methyl group from a substrate. [GOC:mah]
histone demethylase activity	molecular function	Catalysis of the removal of a methyl group from a histone. [GOC:mah]
histone H3K4 demethylase activity	molecular function	Catalysis of the removal of a methyl group from a modified lysine residue at position 4 of the histone H3 protein. [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]
identical protein binding	molecular function	Binding to an identical protein or proteins. [GOC:jl]
MRF binding	molecular function	Binding to Myogenic Regulatory Factor (MRF), a member of the basic Helix-Loop-Helix (bHLH) superfamily of transcription factors. [PMID:10966875]
flavin adenine dinucleotide binding	molecular function	Binding to FAD, flavin-adenine dinucleotide, the coenzyme or the prosthetic group of various flavoprotein oxidoreductase enzymes, in either the oxidized form, FAD, or the reduced form, FADH2. [GOC:ai, GOC:imk, ISBN:0198506732]
nuclear androgen receptor binding	molecular function	Binding to a nuclear androgen receptor. [GOC:ai]
RNA polymerase II-specific DNA-binding transcription factor binding	molecular function	Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw]
telomeric repeat-containing RNA binding	molecular function	Binding to long non-coding RNA molecules transcribed from subtelomeric regions in most eukaryotes. Telomeric repeat-containing RNA (TERRA) molecules consist of subtelomeric-derived sequences and G-rich telomeric repeats. [GOC:BHF, GOC:BHF_telomere, GOC:dph, GOC:jbu, PMID:20655916]
DNA-binding transcription factor binding	molecular function	Binding to a DNA-binding transcription factor, a protein that interacts with a specific DNA sequence (sometimes referred to as a motif) within the regulatory region of a gene to modulate transcription. [GOC:txnOH-2018]
FAD-dependent H3K4me/H3K4me3 demethylase activity	molecular function	Catalysis of the removal of a methyl group from a di- or a monomethyl-lysine residue at position 4 of the histone H3 protein. This is a flavin adenine dinucleotide (FAD)-dependent amine oxidation reaction. [PMID:22473470]
promoter-specific chromatin binding	molecular function	Binding to a section of chromatin that is associated with gene promoter sequences of DNA. [PMID:19948729]
transcription factor binding	molecular function	Binding to a transcription factor, a protein required to initiate or regulate transcription. [ISBN:0198506732]

Located In

This protein is located in 3 target(s):

Target	Category	Definition
chromosome, telomeric region	cellular component	The 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]
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 4 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]
transcription regulator complex	cellular component	A protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl]
protein-containing complex	cellular component	A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah]
DNA repair complex	cellular component	A protein complex involved in DNA repair processes including direct reversal, base excision repair, nucleotide excision repair, photoreactivation, bypass, double-strand break repair pathway, and mismatch repair pathway. [GOC:bhm, PMID:17217467, PMID:20551348, PMID:22749910, PMID:24192350]

Involved In

This protein is involved in 26 target(s):

Target	Category	Definition
negative regulation of transcription by RNA polymerase II	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH]
positive regulation of neuroblast proliferation	biological process	Any process that activates or increases the rate of neuroblast proliferation. [GOC:dph]
regulation of transcription by RNA polymerase II	biological process	Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH]
protein demethylation	biological process	The removal of a methyl group, from a protein amino acid. A methyl group is derived from methane by the removal of a hydrogen atom. [GOC:mah]
positive regulation of epithelial to mesenchymal transition	biological process	Any 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]
positive regulation of neuron projection development	biological process	Any process that increases the rate, frequency or extent of neuron projection development. Neuron projection development is the process whose specific outcome is the progression of a neuron projection over time, from its formation to the mature structure. A neuron projection is any process extending from a neural cell, such as axons or dendrites (collectively called neurites). [GOC:dph, GOC:tb]
cerebral cortex development	biological process	The progression of the cerebral cortex over time from its initial formation until its mature state. The cerebral cortex is the outer layered region of the telencephalon. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid]
negative regulation of protein binding	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of protein binding. [GOC:mah]
neuron maturation	biological process	A developmental process, independent of morphogenetic (shape) change, that is required for a neuron to attain its fully functional state. [GOC:dph, GOC:jl]
negative regulation of DNA binding	biological process	Any process that stops or reduces the frequency, rate or extent of DNA binding. DNA binding is any process in which a gene product interacts selectively with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb]
negative regulation of DNA-binding transcription factor activity	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of the activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:jl]
negative regulation of DNA damage response, signal transduction by p53 class mediator	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of the cascade of processes induced by the cell cycle regulator phosphoprotein p53, or an equivalent protein, in response to the detection of DNA damage. [GOC:jl]
positive regulation of cell size	biological process	Any process that increases cell size. [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]
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]
guanine metabolic process	biological process	The chemical reactions and pathways involving guanine, 2-amino-6-hydroxypurine, a purine that is one of the five main bases found in nucleic acids and a component of a number of phosphorylated guanosine derivatives whose metabolic or regulatory functions are important. [GOC:go_curators]
muscle cell development	biological process	The process whose specific outcome is the progression of a muscle cell over time, from its formation to the mature structure. Muscle cell development does not include the steps involved in committing an unspecified cell to the muscle cell fate. [CL:0000187, GOC:devbiol]
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]
response to fungicide	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 fungicide stimulus. Fungicides are chemicals used to kill fungi. [GOC:dph]
cellular response to cAMP	biological process	Any 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 cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:mah]
regulation of DNA methylation-dependent heterochromatin formation	biological process	Any process that modulates the rate, frequency, or extent of DNA methylation-dependent heterochromatin formation. [GOC:BHF]
positive regulation of cold-induced thermogenesis	biological process	Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809]
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	biological process	Any process that stops, prevents or reduces the frequency, rate or extent of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator. [GOC:TermGenie, PMID:17719541]
positive regulation of neural precursor cell proliferation	biological process	Any process that activates or increases the frequency, rate or extent of neural precursor cell proliferation. [GOC:dph, GOC:yaf]
positive regulation of stem cell proliferation	biological process	Any process that activates or increases the frequency, rate or extent of stem cell proliferation. [GOC:dph]
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]