Lysine-specific demethylase 5A

A lysine-specific demethylase 5A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P29375]

Synonyms

EC 1.14.11.67;
Histone demethylase JARID1A;
Jumonji/ARID domain-containing protein 1A;
Retinoblastoma-binding protein 2;
RBBP-2;
[histone H3]-trimethyl-L-lysine(4) demethylase 5A

Research

Bioassay Publications (15)

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	13 (86.67)	24.3611
2020's	2 (13.33)	2.80

Compounds (15)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
4-hydroxybenzoic acid hydrazide	Homo sapiens (human)	IC50	13.0000	1	1
amiodarone	Homo sapiens (human)	IC50	699.6667	3	3
disulfiram	Homo sapiens (human)	IC50	10.0000	1	1
2,4-pyridinedicarboxylic acid	Homo sapiens (human)	IC50	16.9560	3	10
daminozide	Homo sapiens (human)	IC50	2,200.0000	1	1
di-n-desethylamiodarone	Homo sapiens (human)	IC50	26.0000	2	2
deferasirox	Homo sapiens (human)	IC50	5.0000	1	1
6-ethyl-2,5-dimethyl-7-oxo-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile	Homo sapiens (human)	IC50	0.2370	1	1
oxalylglycine	Homo sapiens (human)	IC50	94.8700	3	11
geldanamycin	Homo sapiens (human)	IC50	0.1300	1	1
17-(dimethylaminoethylamino)-17-demethoxygeldanamycin	Homo sapiens (human)	IC50	0.1300	1	1
tanespimycin	Homo sapiens (human)	IC50	0.1300	1	1
(5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone	Homo sapiens (human)	IC50	20.0000	2	2
3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid	Homo sapiens (human)	IC50	23.2610	3	10
entecavir	Homo sapiens (human)	IC50	20.0000	2	2

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid	Homo sapiens (human)	Kd	12.0000	1	1

Enables

This protein enables 11 target(s):

Target	Category	Definition
transcription cis-regulatory region binding	molecular function	Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH]
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]
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]
enzyme inhibitor activity	molecular function	Binds to and stops, prevents or reduces the activity of an enzyme. [GOC:ai, GOC:ebc]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
zinc ion binding	molecular function	Binding to a zinc ion (Zn). [GOC:ai]
chromatin DNA binding	molecular function	Binding to DNA that is assembled into chromatin. [GOC:mah]
histone demethylase activity	molecular function	Catalysis of the removal of a methyl group from a histone. [GOC:mah]
histone H3K4me/H3K4me2/H3K4me3 demethylase activity	molecular function	Catalysis of the removal of a methyl group from a tri, a di or a monomethyl-lysine residue at position 4 of the histone H3 protein. This is a dioxygenase reaction that is dependent on Fe(II) and 2-oxoglutarate. [PMID:17550896, PMID:22473470]
methylated histone binding	molecular function	Binding to a histone in which a residue has been modified by methylation. [GOC:bf, PMID:14585615]
histone binding	molecular function	Binding to a histone, any of a group of water-soluble proteins found in association with the DNA of eukaryotic or archaeal chromosomes. They are involved in the condensation and coiling of chromosomes during cell division and have also been implicated in gene regulation and DNA replication. They may be chemically modified (methylated, acetlyated and others) to regulate gene transcription. [GOC:jl, PMID:16209651, PMID:30212449, PMID:9305837]

Located In

This protein is located in 3 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]
nucleolus	cellular component	A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732]

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 7 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]
circadian regulation of gene expression	biological process	Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah]
positive regulation of DNA-templated transcription	biological process	Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
regulation of DNA-binding transcription factor activity	biological process	Any process that modulates the frequency, rate or extent of the activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:ai]
facultative heterochromatin formation	biological process	The compaction of chromatin into a conformation that is refactory to transcription but that be converted to euchromatin and allow transcription in specific contexts. These can be temporal (e.g., developmental states or specific cell-cycle stages), spatial (e.g., nuclear localization changes from the center to the periphery or vice versa due to exogenous factors/signals), or parental/heritable (e.g., monoallelic gene expression). [PMID:17936700]
regulation of DNA-templated transcription	biological process	Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
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]