N-lysine methyltransferase KMT5A

An N-lysine methyltransferase KMT5A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NQR1]

Synonyms

EC 2.1.1.-;
H4-K20-HMTase KMT5A;
Histone-lysine N-methyltransferase KMT5A;
2.1.1.361;
Lysine N-methyltransferase 5A;
Lysine-specific methylase 5A;
PR/SET domain-containing protein 07;
PR-Set7;
PR/SET07;
SET domain-cont

Research

Bioassay Publications (6)

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	5 (83.33)	24.3611
2020's	1 (16.67)	2.80

Compounds (5)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
nsc 663284	Homo sapiens (human)	IC50	0.2100	2	2
2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dione	Homo sapiens (human)	IC50	0.4350	2	2
bvt.948	Homo sapiens (human)	IC50	0.7000	2	2
unc 0321	Homo sapiens (human)	IC50	40.0000	1	1
6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine	Homo sapiens (human)	IC50	18.0000	3	3

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
nsc 663284	Homo sapiens (human)	EC50	5.0000	1	1
bvt.948	Homo sapiens (human)	EC50	5.0000	1	1
6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine	Homo sapiens (human)	Kd	27.1500	2	2

Enables

This protein enables 9 target(s):

Target	Category	Definition
transcription corepressor activity	molecular function	A transcription coregulator activity that represses or decreases 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. Corepressors often act by altering chromatin structure and modifications. For example, one class of transcription corepressors 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. [GOC:txnOH-2018, PMID:10213677, PMID:16858867]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
lysine N-methyltransferase activity	molecular function	Catalysis of the transfer of a methyl group from S-adenosyl-L-methionine to the epsilon-amino group of a lysine residue. [GOC:mah]
protein-lysine N-methyltransferase activity	molecular function	Catalysis of the transfer of a methyl group from S-adenosyl-L-methionine to the epsilon-amino group of a lysine residue in a protein substrate. [PMID:12054878]
histone methyltransferase activity	molecular function	Catalysis of the reaction: S-adenosyl-L-methionine + histone = S-adenosyl-L-homocysteine + methyl-histone. Histone methylation generally occurs on either an arginine or a lysine residue. [GOC:curators]
histone H4K20 methyltransferase activity	molecular function	Catalysis of the reaction: S-adenosyl-L-methionine + histone H4 L-lysine (position 20) = S-adenosyl-L-homocysteine + histone H4 N6-methyl-L-lysine (position 20). This reaction is the addition of a methyl group to the lysine residue at position 20 of the histone H4 protein. [PMID:12086618]
histone H4 methyltransferase activity	molecular function	Catalysis of the reaction: Catalysis of the reaction: S-adenosyl-L-methionine + a histone H4 = S-adenosyl-L-homocysteine + a methylated histone H4. Histone methylation generally occurs on either an arginine or a lysine residue. [PMID:28450737]
histone H4K20 monomethyltransferase activity	molecular function	Catalysis of the reaction: L-lysyl20-[histone H4] + S-adenosyl-L-methionine = H+ + N6-methyl-L-lysyl20-[histone H4] + S-adenosyl-L-homocysteine. This reaction is the addition of a methyl group to the unmethylated lysine residue at position 20 of histone H4, producing histone H4K20me. [RHEA:60344]
transcription regulator activity	molecular function	A molecular function that controls the rate, timing and/or magnitude of gene transcription. The function of transcriptional regulators is to modulate gene expression at the transcription step so that they are expressed in the right cell at the right time and in the right amount throughout the life of the cell and the organism. Genes are transcriptional units, and include bacterial operons. [GOC:pg, GOC:txnOH-2018, Wikipedia:Transcription_factor]

Located In

This protein is located in 2 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]
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 2 target(s):

Target	Category	Definition
polytene chromosome	cellular component	A type of chromosome in a polyploid cell, formed when multiple copies of homologous chromosomes are aligned side by side to give a giant chromosome in which distinct chromosome bands are readily visible. [ISBN:0198506732]
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 10 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]
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]
mitotic chromosome condensation	biological process	The cell cycle process in which chromatin structure is compacted prior to and during mitosis in eukaryotic cells. [GOC:mah, ISBN:0815316194]
peptidyl-lysine monomethylation	biological process	The methylation of peptidyl-lysine to form peptidyl-N6-methyl-L-lysine. [RESID:AA0076]
regulation of DNA damage response, signal transduction by p53 class mediator	biological process	Any process that modulates 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]
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]
cell division	biological process	The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr]
regulation of signal transduction by p53 class mediator	biological process	Any process that modulates the frequency, rate or extent of signal transduction by p53 class mediator. [GOC:TermGenie]
negative regulation of double-strand break repair via homologous recombination	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of double-strand break repair via homologous recombination. [GOC:vw]
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]